- Hydroquinone glycosides from leaves of Myrsine seguinii
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From leaves of Myrsine seguinii, seven hydroquinone glycosides were isolated. By spectroscopic analyses, their structures were elucidated to be arbutin, arbutin 2'- and 6'-O-β-apiofuranosides (seguinosides A and B, respectively), and the benzoyl, p-hydroxybenzoyl, 3-methoxy-4-hydroxybenzoyl and 3,5-dimethoxy-4-hydroxybenzoyl esters of the alcohol hydroxyl group on C- 5'' of arbutin 2'-O-β-apiofuranoside (seguinosides C-F, respectively).
- Zhong, Xi-Ning,Otsuka, Hideaki,Ide, Toshinori,Hirata, Eiji,Takushi, Anki,Takeda, Yoshio
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Read Online
- Synthesis, characterization and crystal structure of methyl 4-(benzyloxy)-5-methoxy-2-nitrobenzoate
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Methyl 4-(benzyloxy)-5-methoxy-2-nitrobenzoate was synthesized from 4-hydroxy-3-methoxybenzoic acid. Firstly, 4-hydroxy-3-methoxybenzoic acid reacted with methanol in the presence of concentrated sulfuric acid at reflux temperature, then the product of the first step was transformed into benzyl bromide by the process of substitution reaction by using K2CO3. Finally, the product was obtained by nitration reaction with HNO3. The product was characterized by 1H NMR and LC-MS. The crystal structure of compound I was investigated using X-ray diffraction and SHELXTL-97 software. The results indicated that compound I crystallized in the monoclinic system, space group P2(1)/c with a = 5.590(2), b = 17.591 (7), c = 15.427(6) ?, V = 1516.9 (10) ?3; Z 4.
- Wang, Kai,Zhang, Xiu-Qin,Zhu, Jian,Chen, Qiang,Zhang, Zhong-Qiang,Fan, Li
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Read Online
- Diploquinones A and B, Two New Phytotoxic Tetrasubstituted 1,4-Naphthoquinones from Diplodia mutila, a Causal Agent of Grapevine Trunk Disease
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Two new phytotoxic tetrasubstituted 1,4-naphthoquinones, named diploquinones A and B, were isolated together with vanillic acid from Diplodia mutila (DAR78993), a grapevine pathogen involved in Botryosphaeria dieback in Australia. Diploquinones A and B were characterized as 6,7-dihydroxy-2-methoxy-5-methylnaphthalene-1,4-dione and 3,5,7-trihydroxy-2-methoxynaphthalene-1,4-dione using spectroscopic methods (essentially 1D and 2D 1H and 13C NMR and HR ESIMS). The already known vanillic acid was isolated for the first time as fungal phytotoxin and as metabolite of D. mutila. The three compounds were assayed on detached grapevine leaves (Vitis vinifera cv. Shiraz) at concentrations of 10-3 M and 2.5 × 10-3 M. Vanillic acid showed the highest phytotoxic effect on grapevine leaves irrespective of the tested concentration, while diploquinones A and B showed varying degrees of toxicity.
- Reveglia, Pierluigi,Savocchia, Sandra,Billones-Baaijens, Regina,Masi, Marco,Cimmino, Alessio,Evidente, Antonio
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Read Online
- VISUAL DETECTION OF PBD INDUCED DNA CROSSLINKS
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The present invention relates to the field of oncology, laboratory tools and methods, and especially anti-tumor DNA crosslinking agents. Most patients with advanced solid tumors develop resistance to chemotherapy due to the ability of cancer cells to repair or tolerate sustained DNA damages. The inventors showed that the compounds according to the present invention allow the detection and visualization of alkylated DNA damages induced by PBDs without altering their DNA crosslinking ability. This enables the study of the effect and properties of PBDs. In particular, the present invention relates new derivates of PBD molecules and their synthesis. The present invention also relates to a method for visualizing DNA crosslinking; to a method for assessing the resistance of a tumor to a crosslinking agent and to a method for identifying a molecule or treatment for improving the efficiency of a crosslinking agent.
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Page/Page column 37; 38
(2021/04/23)
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- COMPOSITIONS AND METHODS RELATED TO MOLECULAR CONJUGATION
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The invention relates to activated Michael acceptor (AMA) compounds that can undergo conjugation with biomolecules containing Michael donor moieties, thereby providing plasma-stable antibody-drug conjugates (ADCs). Pharmaceutical compositions of the ADCs are disclosed as well. Also provided herein are a number of applications (e.g., therapeutic applications) in which the compositions are useful.
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Page/Page column 80; 81
(2021/06/11)
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- Transition Metal-Free Regioselective Remote C?H Bond 2,2,2-Trifluoroethoxylation of 8-Aminoquinoline Derivatives at the C5 Position
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The regioselective 2,2,2-trifluoroethoxylation at the C5 position of amides derived from the 8-aminoquinoline has been developed. In the presence of PIDA, an unprecedented and undirected transition metal-free transformation was achieved using the readily available and appealing 2,2,2-trifluoroethanol as the fluorinated source. The selective distal 2,2,2-trifluoroethoxylation of an array of amides was achieved in moderate to good yields (12 examples, up to 61 % yield). This approach provided efficient access to high-value added fluorinated quinoline derivatives, key building blocks for bulk and fine chemical industry.
- Ruyet, Louise,Poisson, Thomas,Besset, Tatiana
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supporting information
p. 3407 - 3410
(2021/06/28)
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- Novel 4-Anilinoquinazoline Derivatives as Potent Anticancer Agents: Design, Synthesis, Cytotoxic Activity, and Docking Study
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The simultaneous inhibition of EGFR and VEGFR-2 is a promising method in cancer treatment. In the present work, several 4-Anilinoquinazoline derivatives encompassing different substitutions at the C-4 and C-7 positions of a quinazoline core were designed, synthesised, and evaluated for their cytotoxicity on A431, HUVEC, and HU02 cell lines. Docking studies were carried out to test the interactions of all synthesised compounds with EGFR and VEGFR-2. Furthermore, a wound healing assay was done for the investigation of cell migration. The most potent compound was 8l followed by the compounds 8i and 8j which showed better cytotoxic activities on A431 and HUVEC cell lines than the standard (Vandetanib). The compounds 8f and 8a represented the best docking energies of 8.99 and 9.35 kcal mol-1 for EGFR and VEGFR, respectively. Moreover, molecular docking studies exhibited that compound 8l showed efficient binding affinity against both EGFR and VEGFR-2. It can bind to these receptors through the formation of essential hydrogen bonds between the quinazoline N1 atom and the Met796 backbone of EGFR and two hydrogen bonds with Cys919 and Thr916 of VEGFR-2 with energies of-7.99 and-7.85 kcal mol-1, respectively. In addition, this compound displayed the highest activity on cell migration and wound healing. Compound 8l with the highest cytotoxic activity can be considered a candidate for further investigation and structural optimisation as an antiproliferative agent.
- Dabirian, Sara,Dogaheh, Mahtab Ghasemi,Ghasemi, Saeed,Moghadam, Fatemeh Azmian,Mojabi, Mohammad,Yousefbeyk, Fatemeh
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p. 730 - 739
(2021/10/29)
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- Design, Synthesis, and Pharmacological Characterization of a Neutral, Non-Prodrug Thrombin Inhibitor with Good Oral Pharmacokinetics
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Despite extensive research on small molecule thrombin inhibitors for oral application in the past decades, only a single double prodrug with very modest oral bioavailability has reached human therapy as a marketed drug. We have undertaken major efforts to identify neutral, non-prodrug inhibitors. Using a holistic analysis of all available internal data, we were able to build computational models and apply these for the selection of a lead series with the highest possibility of achieving oral bioavailability. In our design, we relied on protein structure knowledge to address potency and identified a small window of favorable physicochemical properties to balance absorption and metabolic stability. Protein structure information on the pregnane X receptor helped in overcoming a persistent cytochrome P450 3A4 induction problem. The selected compound series was optimized to a highly potent, neutral, non-prodrug thrombin inhibitor by designing, synthesizing, and testing derivatives. The resulting optimized compound, BAY1217224, has reached first clinical trials, which have confirmed the desired pharmacokinetic properties.
- Hillisch, Alexander,Gericke, Kersten M.,Allerheiligen, Swen,Roehrig, Susanne,Schaefer, Martina,Tersteegen, Adrian,Schulz, Simone,Lienau, Philip,Gnoth, Mark,Puetter, Vera,Hillig, Roman C.,Heitmeier, Stefan
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p. 12574 - 12594
(2020/11/13)
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- FUSED HETEROCYCLIC BENZODIAZEPINE DERIVATIVES AND USES THEREOF
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The present disclosure provides compounds and compositions capable of extending lifespan, and methods of use thereof.
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Page/Page column 85
(2020/05/29)
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- SnCl2 catalyzed direct synthesis of pyrroles under aqueous conditions
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Synthetic substituted pyrroles are related with interesting biological activities, yet they remain inadequately explored within drug discovery. Late years have seen a growing interest in synthetic approaches that can provide access to structurally novel pyrroles so that the biological usefulness of this compound class can be more fully investigated. Herein, an efficient and versatile practical protocol for the pyrroles using stannous(II) chloride dihydrate as catalyst is described under aqueous conditions at 55 oC in high yields. Also, this method is applicable for the preparation of diversity and oriented pyrrole derivatives.
- Tejeswararao,Srikanth
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p. 795 - 802
(2020/03/24)
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- Design, synthesis and biological evaluation of 4-aniline quinazoline derivatives conjugated with hydrogen sulfide (H2S) donors as potent EGFR inhibitors against L858R resistance mutation
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In this study, a series of 4-aniline quinazoline derivatives bearing hydrogen sulfide (H2S) donors were designed, synthesized and evaluated for biological activities. The synthesized compounds were screened for the enzymatic activities against EGFR and EGFR mutants by kinase target-based cell screening method. The results demonstrate that most compounds exhibit selectively inhibitory activities against TEL-EGFR-L858R–BaF3, especially compound 9h with GI50 = 0.008 μM (TEL-EGFR-L858R–BaF3), 0.0069 μM (TEL-EGFR-C797S–BaF3), >10 μM (BaF3), >10 μM (TEL-EGFR-BaF3) and 6.03 μM (TEL-EGFR-T790M-L858R–BaF3). The results from anti-proliferative assays in two NSCLC cell lines indicate that synthetic derivatives (9g, 9h, 15e and 15f) with H2S donor ACS81 display greater anti-proliferative potency against NSCLC cell line H3255 bearing EGFR mutant (L858R) with GI50 values ranging from 0.3486 to 1.348 μM. In addition, compound 9h exhibits weak anti-proliferative effects on other tumor cells (HepG2, MCF-7, HT-29 and A431) and has lower toxic effect on HUVEC cells than AZD9291 (positive control). Meanwhile, compound 9h inhibits the phosphorylation of EGFR in H3255 cells in a dose-dependent manner. Cell cycle analysis reveals that compound 9h suppresses the proliferation of cells by inducing cell cycle arrest in G0-G1 phase. The result of H2S release evaluation suggests that the H2S release of compound 9h is significantly more and faster than other compounds.
- An, Lin,Gao, Cai-Yun,Li, Cheng-Lin,Liu, Yi,Meng, Long,Wu, Xiao-Qing,Xu, Liang,Zhang, Ling,Zhang, Wu-Qi,Zheng, You-Guang
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- NOVEL BENZODIAZEPINE DERIVATIVES AND USES THEREOF
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The present disclosure provides compounds and compositions capable of extending lifespan, and methods of use thereof.
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Paragraph 0502-0504
(2019/12/24)
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- New 4-N-phenylaminoquinoline derivatives as antioxidant, metal chelating and cholinesterase inhibitors for Alzheimer's disease
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A series of new 4-N-phenylaminoquinoline derivatives were designed, synthesized, and their anticholinesterase activities, 1,1-Diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activity, metal-chelating ability were tested. Among them, compounds 11j, 11k and 11l had comparable inhibition activities to reference drug galantamine both in AChE and in BChE. Especially, compound 11j revealed the most potent inhibition to eeAChE and eqBChE with IC50 values of 1.20 μM and 18.52 μM, respectively. Furthermore, both kinetic analysis of AChE inhibition and molecular docking study indicated that compound 11j was mixed-type inhibitor, binding simultaneously to the catalytic anionic site (CAS) and the peripheral anionic site (PAS) of AChE, and propidium iodide displacement assay showed significant displacement of propidium iodide with compound 11k (25.80%) from PAS of eeAChE. More importantly, compound 11l displayed excellent DPPH radical scavenging activity (84% at 1 mg/mL), and its EC50 value was 0.328 μM. In addition, compounds 11a, 11j, 11k and 11l exhibited obvious biometal chelating abilities toward Al3+, Fe2+, Cu2+ and Zn2+ ions. Taken together, 4-N-phenylaminoquinoline derivatives targeting multiple pathogenetic factors deserve further investigation for treatment of AD.
- Cai, Rong,Wang, Li-Ning,Fan, Jing-Jing,Geng, Shang-Qi,Liu, Yu-Ming
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- Synthesis of novel 1,2,3-triazole based polycarboxylic acid functionalised ligands for MOF systems
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Copper catalysed click reactions are excellent tools to generate various 1,2,3-triazole linked polytopic aromatic carboxylates. The general reaction route involves protection of the carboxylates before proceeding with the click reaction. These polycarboxylate azoles are conveniently prepared for potential utility as novel key building blocks for metal organic frameworks. In one case, the ligand crystallises into a solid structure containing 1D, 2D and 3D features, based on a zigzag 1D structure, a ‘chicken mesh’-like 2D structure and a 3D structure with very well-defined channels.
- Belay, Yonas,Coetzee, Louis-Charl,Williams, D. Bradley G.,Muller, Alfred
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supporting information
p. 501 - 503
(2019/01/14)
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- Design, synthesis, evaluation and molecular modeling study of 4-N-phenylaminoquinolines for Alzheimer disease treatment
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Dual binding site acetylcholinesterase (AChE) inhibitors and butyrylcholinesterase (BChE) inhibitors have recently emerged as two classes of new anti-Alzheimer agents to positively modify the disease's course. In this work, a new series of 4-N-phenylaminoquinolines was synthesized and evaluated for their abilities to inhibit AChE and BChE. Compound 11b showed significant inhibitory activities on AChE and BChE with IC50 values of 0.86 and 2.65 μM, respectively, a lot better than that of reference drug galanthamine. Furthermore, docking study showed that compound 11b interacted simultaneously not only with active and peripheral sites of AChE, but also with all five regions of BChE active site. These findings suggest that these derivatives could be regarded as promising starting points for further drug discovery developments.
- Zhu, Jun,Wang, Li-Ning,Cai, Rong,Geng, Shang-Qi,Dong, Ya-Fei,Liu, Yu-Ming
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supporting information
p. 1325 - 1329
(2019/04/08)
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- Design, synthesis and molecular docking studies of quinazolin-4-ones linked to 1,2,3-triazol hybrids as Mycobacterium tuberculosis H37Rv inhibitors besides antimicrobial activity
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Quinazolin-4-ones linked to 1,2,3-triazol (10) were identified as inhibitors of the bisphosphonate BPH-700 transcriptional factor from a high throughput screen. A series of 1,4-disubstituted triazoles (10a–j) were synthesized by the Cu-catalyzed azide-alkyne cyclo addition of 5-methoxy-2-nitro-4-(prop-2-yn-1-yloxy) benzamide (6) with various substituted azido benzenes (7) in the presence of CuSO4 under aerobic conditions followed by click reaction with substituted aldehydes. The target compounds were screened for antitubercular activity against Mycobacterium tuberculosis H37Rv by Broth micro dilution method using Lowenstein Jensen medium (LJ) (MIC 37Rv organism. The study revealed that the target compounds showed good affinity toward the protein when compared to the standard drug Pefloxacin. Further, 10b was found to interact with three amino acids, viz., Gln92, Arg200, Ser196, as evidenced by the large interaction energy (ΔG = ?8.16 kcal/mol). Besides the above, the synthesized quinazolinone triazoles 10a–j were evaluated for their antibacterial activities against a panel of Gram +ve and Gram –ve bacteria. Among them 10a, 10e, 10 h and 10j showed promising broad spectrum antibacterial activity with inhibition in the range of 19–33-mm diameter of inhibition zone (DIZ).
- Maddali, Narendra Kumar,Viswanath, I. V. Kasi,Murthy,Bera, Rabin,Takhi, Mohamed,Rao, Nethinti Sundara,Gudla, Vanajakshi
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p. 559 - 570
(2019/03/14)
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- Oxidative cleavage of β-O-4 bonds in lignin model compounds with a single-atom Co catalyst
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Single-atom catalysts are emerging as primary catalysts for many reactions due to their 100% utilization of active metal centers leading to high catalytic efficiencies. Herein, we report the use of a single-atom Co catalyst for the oxidative cleavage of the β-O-4 bonds of lignin model compounds at a low oxygen pressure. Under the optimized reaction conditions, the conversion of 2-(2-methoxyphenoxy)-1-phenylethanol up to 95% with high selectivities was achieved with a variety of substrates investigated. The reusability of the Co catalyst with a high catalytic efficiency indicates its potential application in the oxidative cleavage of C-O bonds.
- Liu, Sijie,Bai, Lichen,Van Muyden, Antoine P.,Huang, Zhangjun,Cui, Xinjiang,Fei, Zhaofu,Li, Xuehui,Hu, Xile,Dyson, Paul J.
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supporting information
p. 1974 - 1981
(2019/04/29)
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- Antifungal activity of cinnamic acid and benzoic acid esters against Candida albicans strains
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Candida albicans is an important opportunistic fungal pathogen capable of provoking infection in humans. In the present study, we evaluated the antifungal effect of 23 ester derivatives of the cinnamic and benzoic acids against 3 C. albicans strains (ATCC-76645, LM-106 and LM-23), as well as discuss their Structure–Activity Relationship (SAR). The antifungal assay results revealed that the screened compounds exhibited different levels of activity depending on structural variation. Among the ester analogues, methyl caffeate (5) and methyl 2-nitrocinnamate (10) were the analogues that presented the best antifungal effect against all C. albicans strains, presenting the same MIC values (MIC?=?128?μg/mL), followed by methyl biphenyl-2-carboxylate (21) (MIC?=?128, 128 and 256?μg/mL for C. albicans LM-106, LM-23, and ATCC-76645, respectively). Our results suggest that certain molecular characteristics are important for the antifungal action.
- Lima, Tamires C.,Ferreira, Alana R.,Silva, Daniele F.,Lima, Edeltrudes O.,de Sousa, Dami?o P.
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p. 572 - 575
(2017/09/30)
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- Synthesis of 4-N-anilinoquinoline compounds and application in preparation of anti-Alzheimer's disease drugs
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The invention discloses synthesis of 4-N-anilinquinoline compounds and application in preparation of anti-Alzheimer's disease drugs. The synthesis method comprises taking acetone as a solvent, dissolving 6-methoxy-7-(3-chloropropoxy)-3-nitro-4-N-substituted anilinoquinoline, dropwise adding morpholine, and then performing heating for a reaction, after the reaction is finished, performing cooling to room temperature, and performing drying and purification to obtain the target compound. The 4-N-anilinquinoline compounds include nine kinds of compounds, and the nine kinds of compounds have dual inhibitory activity on acetylcholinesterase and butyrylcholinesterase, have appropriate lipophilicity, can be used to prepare anti-Alzheimer's drugs, and open up a new way for development of novel drugs for treating Alzheimer's disease.
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Paragraph 0025; 0026; 0027
(2018/04/03)
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- Structural design, synthesis and substituent effect of hydrazone-N-acylhydrazones reveal potent immunomodulatory agents
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4-(Nitrophenyl)hydrazone derivatives of N-acylhydrazone were synthesized and screened for suppress lymphocyte proliferation and nitrite inhibition in macrophages. Compared to an unsubstituted N-acylhydrazone, active compounds were identified within initial series when hydroxyl, chloride and nitro substituents were employed. Structure-activity relationship was further developed by varying the position of these substituents as well as attaching structurally-related substituents. Changing substituent position revealed a more promising compound series of anti-inflammatory agents. In contrast, an N-methyl group appended to the 4-(nitrophenyl)hydrazone moiety reduced activity. Anti-inflammatory activity of compounds is achieved by modulating IL-1β secretion and prostaglandin E2 synthesis in macrophages and by inhibiting calcineurin phosphatase activity in lymphocytes. Compound SintMed65 was advanced into an acute model of peritonitis in mice, where it inhibited the neutrophil infiltration after being orally administered. In summary, we demonstrated in great details the structural requirements and the underlying mechanism for anti-inflammatory activity of a new family of hydrazone-N-acylhydrazone, which may represent a valuable medicinal chemistry direction for the anti-inflammatory drug development in general.
- Meira, Cássio S.,dos Santos Filho, José Maurício,Sousa, Caroline C.,Anjos, Pamela S.,Cerqueira, Jéssica V.,Dias Neto, Humberto A.,da Silveira, Rafael G.,Russo, Helena M.,Wolfender, Jean-Luc,Queiroz, Emerson F.,Moreira, Diogo R.M.,Soares, Milena B.P.
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p. 1971 - 1985
(2018/03/12)
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- Molecularly imprinted artificial esterases with highly specific active sites and precisely installed catalytic groups
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A difficult challenge in synthetic enzymes is the creation of substrate-selective active sites with accurately positioned catalytic groups. Covalent molecular imprinting in cross-linked micelles afforded such active sites in protein-sized, water-soluble nanoparticle catalysts. Our method allowed a systematic tuning of the distance of the catalytic group to the bound substrate. The catalysts displayed enzyme-like kinetics and easily distinguished substrates with subtle structural differences.
- Hu, Lan,Zhao, Yan
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supporting information
p. 5580 - 5584
(2018/08/17)
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- Compound TVA-X having neuroprotection effect, preparation method and applications thereof
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The invention relates to a compound TVA-X having neuroprotection effect, a preparation method and applications thereof, and provides a class of compounds having a structure general formula 1, and a preparation method thereof, and applications in preparation of drugs for treatment of brain nerve injury and sequela thereof, wherein the composition can significantly protect cobalt chloride induced PC12 cell damage, wherein the compound VA-06 has strong protection effect on cobalt chloride induced PC12 cell damage compared to the positive drug ligustrazine. The formula 1 is defined in the specification.
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Paragraph 0041; 0042; 0072; 0073
(2018/09/14)
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- Process for preparing biphenyl compounds
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The present invention relates to a process for preparing a compound having the formula (I), said process comprising the following steps: a) the addition of an oxygen source into a solution of a compound of formula (II), in a water-miscible solvent, b) the addition of a laccase in the solution obtained after step a); and c) the possible recovering of the compound of formula (I) thus obtained.
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Page/Page column 20; 21
(2019/01/04)
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- A biocatalytic method for the chemoselective aerobic oxidation of aldehydes to carboxylic acids
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Herein, we present a study on the oxidation of aldehydes to carboxylic acids using three recombinant aldehyde dehydrogenases (ALDHs). The ALDHs were used in purified form with a nicotinamide oxidase (NOx), which recycles the catalytic NAD+ at the expense of dioxygen (air at atmospheric pressure). The reaction was studied also with lyophilised whole cell as well as resting cell biocatalysts for more convenient practical application. The optimised biocatalytic oxidation runs in phosphate buffer at pH 8.5 and at 40 °C. From a set of sixty-one aliphatic, aryl-Aliphatic, benzylic, hetero-Aromatic and bicyclic aldehydes, fifty were converted with elevated yield (up to >99%). The exceptions were a few ortho-substituted benzaldehydes, bicyclic heteroaromatic aldehydes and 2-phenylpropanal. In all cases, the expected carboxylic acid was shown to be the only product (>99% chemoselectivity). Other oxidisable functionalities within the same molecule (e.g. hydroxyl, alkene, and heteroaromatic nitrogen or sulphur atoms) remained untouched. The reaction was scaled for the oxidation of 5-(hydroxymethyl)furfural (2 g), a bio-based starting material, to afford 5-(hydroxymethyl)furoic acid in 61% isolated yield. The new biocatalytic method avoids the use of toxic or unsafe oxidants, strong acids or bases, or undesired solvents. It shows applicability across a wide range of substrates, and retains perfect chemoselectivity. Alternative oxidisable groups were not converted, and other classical side-reactions (e.g. halogenation of unsaturated functionalities, Dakin-Type oxidation) did not occur. In comparison to other established enzymatic methods such as the use of oxidases (where the concomitant oxidation of alcohols and aldehydes is common), ALDHs offer greatly improved selectivity.
- Knaus, Tanja,Tseliou, Vasilis,Humphreys, Luke D.,Scrutton, Nigel S.,Mutti, Francesco G.
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p. 3931 - 3943
(2018/09/11)
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- Study of new synthesized ferrocenyl ionic liquids in oxidative esterification reaction
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In this work, novel ferrocene-based ionic liquids, 1-(ferrocenylbutyl)-4-(3-methylimidazolium) Azide and 1-(ferrocenylbutyl)-4-(3-methylimidazolium) Tetrafluoroborate, were synthesized and utilized in the oxidation esterification reaction of aldehydes in the present of different reagents such as NaN3, (K2CO3 and NCS), (KI and KCN), (I2 and K2CO3), (KMnO4). The results were compared with that of [BMIM][X] (X?Cl, BF4) under the same conditions. As expected, ferrocene-based ionic liquids showed better results; It seems, iron nuclear may play a similar role such as iron catalysts in these novel ionic liquids and can facilitated the oxidation esterification reaction with improve the yield and decrease the reaction time.
- Teimuri-Mofrad, Reza,Rahimpour, Keshvar,Rezaei, Hannaneh,Valizadeh, Hassan,Aghaiepour, Alireza
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p. 1425 - 1435
(2018/04/05)
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- Palladium-Catalyzed Aerobic Oxidative Carbonylation of C–H Bonds in Phenols for the Synthesis of p-Hydroxybenzoates
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This work reports the synthesis of p-hydroxybenzoates directly from phenols by oxidative carbonylation of phenolic C–H bonds, proceding through oxidative iodination. The developed methodology is efficient and economically attractive because phenols are cheap and easily available starting materials. This one-pot strategy was expediently applied to the synthesis of a variety of p-hydroxybenzoates by utilizing simple primary and secondary alcohols with different phenols under mild reaction conditions. Advantageously, the procedure has no need for co-catalysts, co-solvents or external ligands. The utilization of molecular oxygen as a terminal oxidant for C–H bond oxidation represents an additional benefit.
- Gaikwad, Vinayak V.,Bhanage, Bhalchandra M.
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p. 2877 - 2881
(2018/06/21)
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- NOVEL MANUFACTURING METHOD OF LOW MOLECULAR COMPOUND FROM LIGNIN
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PROBLEM TO BE SOLVED: To provide a manufacturing method of dehydro divanillic acid dialkyl ester using lignin contained in a needle-leaves trees or the like as a raw material. SOLUTION: The manufacturing method of dehydro divanillic acid dialkyl ester through following process 1 to process 5 with using lignin as a raw material. Process 1: a process for conducting an oxidation reaction on the lignin. Process 2: a process for purifying a reaction product obtained in the process 1. Process 3: a process for conducting the oxidation reaction on a component obtained in the process 2. Process 4: a process for conducting an esterification reaction on a reaction product of the process 3 and alcohol. Process 5: a process for conducting a coupling reaction (dimerization reaction) on a reaction product in the process 4. SELECTED DRAWING: None COPYRIGHT: (C)2017,JPOandINPIT
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Paragraph 0058
(2018/02/10)
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- Partially bio-based poly(amide imide)s by polycondensation of aromatic diacylhydrazides based on lignin-derived phenolic acids and aromatic dianhydrides: Synthesis, characterization, and computational studies
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Two new bio-based diacylhydrazide monomers, namely, 4,4′-(propane-1,3-diylbis(oxy))bis(3-methoxybenzohydrazide) and 4,4′-(propane-1,3-diylbis(oxy))bis(3,5-dimethoxybenzohydrazide) were synthesized starting from lignin-derived phenolic acids, namely, vanillic acid and syringic acid. A series of poly(amide imide)s was synthesized by polycondensation of these diacylhydrazide monomers with commercially available aromatic dianhydrides. Poly(amide imide)s showed inherent viscosity in the range 0.44–0.56 dL?g?1 and exhibited good solubility in organic solvents. Poly(amide imide)s could be cast into transparent, flexible, and tough films from their N,N-dimethylacetamide solutions. Poly(amide imide)s showed 10% weight loss in the temperature range 340–364?°C indicating their good thermal stability. Glass transition temperature (Tg) of poly(amide imides)s were measured by DSC and DMA which were in the range 201–223?°C and 214–248?°C, respectively. The Tg values of poly(amide imide)s were dependent on the number methoxy substituents on aromatic rings of diacylhydrazide monomers. Molecular dynamics simulation studies revealed that chain rigidity is the dominant factor for observed trends in Tg.
- Kuhire, Sachin S.,Sharma, Pragati,Chakrabarty, Suman,Wadgaonkar, Prakash P.
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p. 3636 - 3645
(2017/10/31)
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- Synthesis and cytotoxic activity of 4-O-β-D-galactopyranosyl derivatives of phenolic acids esters
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The glycosylation of naturally occurring phenolic acids has a significant impact on their solubility, stability and physiochemical properties. D-Galactose residue was found to form a part of glycoconjugates in several tissues and involved in a variety of physiological process. To the best of our knowledge, we have noticed a little information about the glycosylation of the phenolic acids with galactose residue. In this work, we describe the glycosylation of methyl vanillate and methyl ferulate with peracetylated-β-D-galactopyranose in the presence of BF3·OEt2. The coupling reaction yielded efficiently and selectively only the acetylated β-D-galactopyranosides 3 and 6. Removal of the acetyl groups using sodium methoxide afforded the corresponding β-D-galactopyranosides 4 and 7 in good yields. Anticancer activity in vitro was evaluated against two human cancer cell lines (MCF-7 breast cancer cell lines and PC-3 prostate cancer cell lines). β-D-galactopyranosides 4 and 7 demonstrated improved cytotoxic activity compared to the parental esters.
- Al Bujuq, Nader,Arar, Sharif,Khalil, Raida
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supporting information
p. 1 - 7
(2017/10/07)
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- Composition FOR PREVENTING ALOPECIA AND ACTIVATING HAIR GROWTH
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The present invention provides a hair growth promoter comprising as an active ingredient, a compound having a chemical structure of general formula (1) or a pharmacologically acceptable salt thereof. In the general formula (1): R_1 is a saturated or unsaturated straight chain or branched C1-C10 alkyl group or hydroxy alkyl group; R_2 is hydrogen or a saturated or unsaturated straight chain or branched C1-C10 alkoxy or hydroxy alkoxy; X is hydrogen, hydroxy, or a saturated or unsaturated straight chain or branched C1-C10 alkyl group, alkoxy or hydroxyl alkoxy; R_3 and R_4 are each independently selected from R_5, hydrogen, aldehyde, and a saturated or unsaturated straight chain or branched alkyl, alkoxy, or hydroxy alkoxy; R_5 has a structure of # AAA #; R_6 is selected from hydrogen, and a saturated or unsaturated straight chain or branched C1-C10 alkyl, alkoxy, or hydroxy alkoxy; and one of R_3 and R_4 is hydrogen.COPYRIGHT KIPO 2017
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Paragraph 0204; 0212; 0213
(2018/02/16)
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- 1-substituted 4-arylpiperazine as kappa opioid receptor antagonists
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Provided are compounds represented by the formula: where R, Y3, R1, R2, R3, R4, R6, G, R7, E1, E2, A, B, W, X, Y and Z are as defined herein.
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Page/Page column 26-27
(2016/12/26)
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- Novel diether compounds inhibiting differentiation of osteoclasts
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Osteoporosis is a disorder in which bone mass decreases and is responsible for many degenerative bone diseases. The excessive formation and activity of osteoclasts results in pathological disorders of the bone. Receptor Activator of Nuclear Factor κB Ligand (RANKL) is regarded as a key regulator of osteoclast activity and as a new therapeutic target for treating osteoporosis. Herein, we have synthesized several new small molecules and tested their inhibition activity on RANKL-induced osteoclast formation. The active compounds 2c and 4d showed inhibitory activity against RANKL-induced osteoclast differentiation (IC50 = 1.56 and 2.20 μM, respectively). The most active compound 2c prevented LPS-induced osteoclastogenesis in vivo. These data imply that the compound may be the potential candidate for a new therapeutic drug for treatment of bone resorption-associated diseases.
- Doh, Kyung Eun,Kang, Ju-Hee,Ting, Zheng,Yim, Mijung,Choo, Hea-Young Park
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p. 178 - 190
(2016/03/12)
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- Selective laccase-catalyzed dimerization of phenolic compounds derived from lignin: Towards original symmetrical bio-based (bis) aromatic monomers
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A laccase-catalyzed process was developed to prepare, selectively, in high yield, dimers of lignin-based phenolic compounds without any purification. The influence of experimental parameters such as laccase loading, nature of solvent and the presence of oxygen on the conversion of vanillin was investigated. After the dimerization, the product obtained as a precipitate is filtered off and the solution containing the enzyme can be re-used several times, which improves the process economics. A phenolic-substrate screening reveals that such process enables to dimerize regioselectively, six ortho-methoxy-para-substituted phenols (vanillin, 4-hydroxy-3-methoxybenzonitrile, acetovanillon, methyl vanillate, 2-methoxy-4-methylphenol, and eugenol) with yields ranging from 87% to 96% and one ortho-disubstituted phenol (2,6-dimethoxyphenol) with 80% yield.
- Llevot, Audery,Grau, Etienne,Carlotti, Stéphane,Grelier, Stéphane,Cramail, Henri
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- H2S donor compound based on quinazoline structure and application thereof
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The invention discloses an H2S donor compound based on a quinazoline structure and an application thereof. The H2S donor compound is a compound shown as a formula (I) or a pharmaceutically-acceptable salt thereof, wherein Ar is substituted or unsubstituted phenyl, and a substituent thereof is selected from one or more of halogen, nitro, C1-C4 alkyl, halogenated C1-C4 alkyl, alkoxy with 1-4 carbon atoms and halogenated alkoxy with 1-4 carbon atoms; X is alkoxy with 1-4 carbon atoms, a B-NH or A-CH2CO-NH- group; Y is a H, B-CnH2nO- or A-CnH2nO- group; A or B is a H2S donor group; n is an integer being 1-5; Y is not H when X is alkoxy with 1-3 carbon atoms. A series of H2S donor compounds based on a 4-anilino quinazoline structure are designed and synthesized, and the antineoplastic activity of a medicament is increased under the synergistic action of H2S and 4-anilino quinazoline derivatives. The formula of the H2S donor compound is shown in the description.
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Paragraph 0085; 0086; 0087
(2017/07/20)
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- Benzamide capped peptidomimetics as non-ATP competitive inhibitors of CDK2 using the REPLACE strategy
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Inhibition of cyclin dependent kinase 2 (CDK2) in complex with cyclin A in G1/S phase of the cell cycle has been shown to promote selective apoptosis of cancer cells through the E2F1 pathway. An alternative approach to catalytic inhibition is to target the substrate recruitment site also known as the cyclin binding groove (CBG) to generate selective non-ATP competitive inhibitors. The REPLACE strategy has been applied to identify fragment alternatives and substituted benzoic acid derivatives were evaluated as a promising scaffold to present appropriate functionality to mimic key peptide determinants. Fragment Ligated Inhibitory Peptides (FLIPs) are described which potently inhibit both CDK2/cyclin A and CDK4/cyclin D1 and have preliminary anti-tumor activity. A structural rationale for binding was obtained through molecular modeling further demonstrating their potential for further development as next generation non ATP competitive CDK inhibitors.
- Premnath, Padmavathy Nandha,Craig, Sandra N.,Liu, Shu,McInnes, Campbell
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supporting information
p. 3754 - 3760
(2016/07/22)
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- Chemoselective dehydrogenative esterification of aldehydes and alcohols with a dimeric rhodium(II) catalyst
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Dehydrogenative cross-coupling of aldehydes with alcohols as well as dehydrogentive cross-coupling of primary alcohols to produce esters have been developed using a Rh-terpyridine catalyst. The catalyst demonstrates broad substrate scope and good functional group tolerance, affording esters highly selectively. The high chemoselectivity of the catalyst stems from its preference for dehydrogenation of benzylic alcohols over aliphatic ones. Preliminary mechanistic studies suggest that the active catalyst is a dimeric Rh(ii) species, operating via a mechanism involving metal-base-metal cooperativity.
- Cheng, Junjie,Zhu, Meijuan,Wang, Chao,Li, Junjun,Jiang, Xue,Wei, Yawen,Tang, Weijun,Xue, Dong,Xiao, Jianliang
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p. 4428 - 4434
(2016/07/07)
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- Water-Soluble molecularly imprinted nanoparticles (MINPs) with tailored, functionalized, modifiable binding pockets
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Construction of receptors with binding sites of specific size, shape, and functional groups is important to both chemistry and biology. Covalent imprinting of a photocleavable template within surface-core doubly cross-linked micelles yielded carboxylic acid-containing hydrophobic pockets within the water-soluble molecularly imprinted nanoparticles. The functionalized binding pockets were characterized by their binding of amine- and acid-functionalized guests under different pH values. The nanoparticles, on average, contained one binding site per particle and displayed highly selective binding among structural analogues. The binding sites could be modified further by covalent chemistry to modulate their binding properties.
- Awino, Joseph K.,Zhao, Yan
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supporting information
p. 655 - 661
(2015/08/04)
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- Computational and Experimental Studies of Phthaloyl Peroxide-Mediated Hydroxylation of Arenes Yield a More Reactive Derivative, 4,5-Dichlorophthaloyl Peroxide
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The oxidation of arenes by the reagent phthaloyl peroxide provides a new method for the synthesis of phenols. A new, more reactive arene oxidizing reagent, 4,5-dichlorophthaloyl peroxide, computationally predicted and experimentally determined to possess enhanced reactivity, has expanded the scope of the reaction while maintaining a high level of tolerance for diverse functional groups. The reaction proceeds through a novel "reverse-rebound" mechanism with diradical intermediates. Mechanistic insight was achieved through isolation and characterization of minor byproducts, determination of linear free energy correlations, and computational analysis of substituent effects of arenes, each of which provided additional support for the reaction proceeding through the diradical pathway.
- Camelio, Andrew M.,Liang, Yong,Eliasen, Anders M.,Johnson, Trevor C.,Yuan, Changxia,Schuppe, Alex W.,Houk,Siegel, Dionicio
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p. 8084 - 8095
(2015/09/01)
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- CYCLIC PEROXIDE OXIDATION OF AROMATIC COMPOUND PRODUCTION AND USE THEREOF
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The present invention provides a method for converting an aromatic hydrocarbon to a phenol by providing an aromatic hydrocarbon comprising one or more aromatic C-H bonds and one or more activated C-H bonds in a solvent; adding a phthaloyl peroxide to the solvent; converting the phthaloyl peroxide to a di-radical; contacting the di-radical with the one or more aromatic C-H bonds; oxidizing selectively one of the one or more aromatic C-H bonds in preference to the one or more activated C-H bonds; adding a hydroxyl group to the one of the one or more aromatic C-H bonds to form one or more phenols; and purifying the one or more phenols.
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Page/Page column 10
(2014/10/15)
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- 1-SUBSTITUTED 4-ARYLPIPERAZINE AS KAPPA OPIOID RECEPTOR ANTAGONISTS
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Provided are compounds represented by the formula: where R, Y3, R1,R2, R3, R4, R6, G, R7, E1, E2, A, B, W, X, Y and Z are as defined herein.
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Page/Page column 34
(2013/06/27)
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- NEW COMPOUNDS FOR ALLEVIATION, PREVENTION OR TREATMENT OF OSTEOPOROSIS, THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
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The present invention provides novel compounds of Chemical Formula I, a pharmaceutically acceptable salt thereof, or a hydrate or solvate thereof, a preparation thereof and a composition for the alleviation, prevention or treatment of osteoporosis, comprising thereof in an effective amount, and a method for alleviating, preventing or treating osteoporosis.
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Paragraph 0208
(2013/03/26)
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- Discovery of N-{4-[(3-hydroxyphenyl)-3-methylpiperazin-1-yl]methyl-2- methylpropyl}-4-phenoxybenzamide analogues as selective kappa opioid receptor antagonists
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There is continuing interest in the discovery and development of new κ opioid receptor antagonists. We recently reported that N-substituted 3-methyl-4-(3-hydroxyphenyl)piperazines were a new class of opioid receptor antagonists. In this study, we report the syntheses of two piperazine JDTic-like analogues. Evaluation of the two compounds in an in vitro [35S] GTPγS binding assay showed that neither compound showed the high potency and κ opioid receptor selectivity of JDTic. A library of compounds using the core scaffold 21 was synthesized and tested for their ability to inhibit [35S]GTPγS binding stimulated by the selective κ opioid agonist U69,593. These studies led to N-[(1S)-1-{[(3S)-4-(3-hydroxyphenyl)-3- methylpiperazin-1-yl]methyl}-2-methylpropyl]-4-phenoxybenzamide (11a), a compound that showed good κ opioid receptor antagonist properties. An SAR study based on 11a provided 28 novel analogues. Evaluation of these 28 compounds in the [35S]GTPγS binding assay showed that several of the analogues were potent and selective κ opioid receptor antagonists.
- Kormos, Chad M.,Jin, Chunyang,Cueva, Juan Pablo,Runyon, Scott P.,Thomas, James B.,Brieaddy, Lawrence E.,Mascarella, S. Wayne,Navarro, Hernán A.,Gilmour, Brian P.,Carroll, F. Ivy
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p. 4551 - 4567
(2013/07/19)
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- Chemical interaction between polyphenols and a cysteinyl thiol under radical oxidation conditions
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Chemical interaction between polyphenols and thiols was investigated under radical oxidation conditions using a model cysteinyl thiol derivative, N-benzoylcysteine methyl ester. The radical oxidation was carried out with a stoichiometric amount of 2,2-diphenyl-1-picrylhydrazyl (DPPH), and the decreases in the amounts of polyphenols and the thiol were measured by HPLC analysis. Cross-coupling products between various polyphenols and the thiol were examined by LC-MS in reactions that showed decreases in both the polyphenols and the thiol. The LC-MS results indicated that three phenolic acid esters (methyl caffeate, methyl dihydrocaffeate, and methyl protocatechuate) and six flavonoids (kaempferol, myricetin, luteolin, morin, taxifolin, and catechin) gave corresponding thiol adducts, whereas three polyphenols (methyl ferulate, methyl sinapate, and quercetin) gave only dimers or simple oxidation products without thiol substituents. Thiol adducts of the structurally related compounds methyl caffeate and methyl dihydrocaffeate were isolated, and their chemical structures were determined by NMR analysis. The mechanism for the thiol addition was discussed on the basis of the structures of the products.
- Fujimoto, Aya,Masuda, Toshiya
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experimental part
p. 5142 - 5151
(2012/10/07)
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- Design, synthesis and antibacterial activities of vanillic acylhydrazone derivatives as potential β-ketoacyl-acyl carrier protein synthase III (FabH) inhibitors
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Fatty acid biosynthesis is essential for bacterial survival. FabH, β-ketoacyl-acyl carrier protein (ACP) synthase III, is a particularly attractive target, since it is central to the initiation of fatty acid biosynthesis and is highly conserved among Gram-positive and Gram-negative bacteria. A series of acylhydrazone derivatives were synthesized and developed as potent inhibitors of FabH. This inhibitor class demonstrates strong broad-spectrum antibacterial activity. Compounds with potent antibacterial activities were tested for their Escherichia coli FabH inhibitory activity. Especially, compound E9 showed the most potent antibacterial activity with MIC values of 0.39-1.56 μg/mL against the tested bacterial strains and exhibited the most potent E. coli FabH inhibitory activity with IC50 of 2.5 μM. Docking simulation was performed to position compound E9 into the E. coli FabH active site to determine the probable binding conformation.
- Wang, Xiao-Liang,Zhang, Yan-Bin,Tang, Jian-Feng,Yang, Yu-Shun,Chen, Ruo-Qi,Zhang, Fei,Zhu, Hai-Liang
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p. 373 - 382
(2013/01/15)
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- Synthesis of bosutinib from 3-methoxy-4-hydroxybenzoic acid
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This paper reports a novel synthesis of bosutinib starting from 3-methoxy-4-hydroxybenzoic acid. The process starts with esterification of the starting material, followed by alkylation, nitration, reduction, cyclization, chlorination and two successive amination reactions. The intermediates and target molecule were characterized by 1H-NMR, 13C-NMR, MS and the purities of all the compounds were determined by HPLC.
- Yin, Xiao Jia,Xu, Guan Hong,Sun, Xu,Peng, Yan,Ji, Xing,Jiang, Ke,Li, Fei
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experimental part
p. 4261 - 4266
(2010/09/18)
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- METHOD FOR THE BREAKDOWN OF LIGNIN
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The invention describes a method for the direct production of molecules with a minimum molecular weight of 78 g/mol by the breakdown of lignin, lignin derivatives, lignin fragments, and/or lignin-containing substances or mixtures in the presence of at least one polyoxometallate and preferably in the presence of a radical scavenger in a liquid medium.
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Page/Page column 5-8
(2010/06/11)
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- A selective de-O-methylation of guaiacyl lignans to corresponding catechol derivatives by 2-iodoxybenzoic acid (IBX). the role of the catechol moiety on the toxicity of lignans
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We report here the first selective de-O-methylation of a large panel of guaiacyl lignans to the corresponding catechol derivatives by using IBX as primary oxidant under green conditions (dimethyl carbonate-H2O solvent) through an in situ reduction procedure. The influence of the catechol moiety on the cytotoxicity and genotoxicity of new lignan derivatives has been investigated. The results obtained indicated that the presence of the catechol moiety sharply enhances the clastogenic potential (e.g. induction of chromosomal aberrations), the cytotoxicity and the modulation of cell cycle progression with respect to the parent compounds. Thus, despite the in vitro antioxidant activity usually described for catechol derivatives, our results show for the first time the generation of a clastogenic potential, highly indicative of a long-term genetic and cancer risk. The Royal Society of Chemistry 2009.
- Bernini, Roberta,Barontini, Maurizio,Mosesso, Pasquale,Pepe, Gaetano,Willfoer, Stefan M.,Sjoeholm, Rainer E.,Eklund, Patrik C.,Saladino, Raffaele
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scheme or table
p. 2367 - 2377
(2009/09/26)
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- Towards the development of a covalently tethered MALDI system - A study of allyl-modified MALDI matrixes
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An emerging application of matrix-assisted laser desorption ionization (MALDI) mass spectrometry is the analysis of low molecular weight (LMW) compounds, often via coupled, liquid chromatography - MALDI-MS methods. However, in many cases, the low molecular weight region of MALDI mass spectra is obscured by the presence of signals originating from the matrix, suggesting that the development of tethered MALDI matrixes may be required to optimize MS performance for such compounds. To gain insight into potential sites for covalent attachment of MALDI matrixes, we have systematically investigated the role played by a variety of functional group motifs in determining matrix efficiency for three common MALDI matrixes, as judged both by total signal intensity and background noise from matrix decomposition for a set of LMW compounds. A series of allyl derivatives of standard matrixes was prepared, and the efficiency of these materials in the MALDI experiment was measured. All modifications of established matrixes, e.g., 2,5-dihydroxybenzoic acid (DHB), α-cyano-4-hydroxycinnamic acid (CHCA), and caffeic acid (CA), or close analogues led to decreased absolute signal intensity and signal-to-background levels. Improved performance was generally observed with (i) the presence of a phenolic group (carboxylic acids were less effective) (ii) crystalline derivatives, and (iii) compounds that had high extinction coefficients at wavelengths near to that of the exciting laser (337 nm). The most interesting derivatives were the O-allyl ether (15) and N-allyl amide (16) of caffeic acid. These compounds did not facilitate signals from all four analytes tested. However, the observed spectra contained fewer signals from the matrix than from the parent compound CA. These compounds demonstrate that functionalization of MALDI matrixes, ultimately leading to tethered matrixes, is possible without jeopardizing signal intensity.
- Martic, Sanela,Brennan, John D.,Brook, Michael A.,Ackloo, Suzanne,Nagy, Noemi
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- Chemical defense of the crust fungus Aleurodiscus amorphus by a tailor-made cyanogenic cyanohydrin ether
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(Chemical Equation Presented) A mighty midget! When injured, the crust fungus A. amorphus (left in the picture) releases hydrocyanic acid by an oxidative mechanism so far unknown in nature. In contrast to cyanogenic glycosides in which the smooth hydrolysis of the glycoside bond is essential for the liberation of hydrocyanic acid, in aleurodisconitrile the oxidation-prone aromatic moiety enables the release of hydrocyanic acid.
- Kindler, Bernhard L. J.,Spiteller, Peter
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p. 8076 - 8078
(2008/09/17)
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- In vitro inhibitory activity of boropinic acid against Helicobacter pylori
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In this study, we assessed in vitro minimum inhibitory concentration (MIC) values of some natural geranyloxycoumarins, geranyloxy- and isopentenyloxy acids against growth of Helicobacter pylori. Boropinic acid, active principle isolated from Boronia pinnata (Fam. Rutaceae), was seen to be the most effective compound with a MIC value of 1.62 μg/mL.
- Epifano, Francesco,Menghini, Luigi,Pagiotti, Rita,Angelini, Paola,Genovese, Salvatore,Curini, Massimo
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p. 5523 - 5525
(2007/10/03)
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- SUBSTITUTED N-ARYL BENZAMIDES AND RELATED COMPOUNDS FOR TREATMENT OF AMYLOID DISEASES AND SYNUCLEINOPATHIES
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Substituted diaryl compounds of the Formulae (I, II, III), where the variables are as defined in the claims, and their pharmaceutically acceptable derivatives, their synthesis, pharmaceutical compositions containing them, and their use in the treatment of amyloid diseases, including A? amyloidosis, such as observed in Alzheimer's disease, IAPP amyloidosis, such as observed in type 2 diabetes, and synucleinopathies, such as observed in Parkinson's disease, and the manufacture of medicaments for such treatment are provided.
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Page/Page column 92-93
(2008/06/13)
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