- EBNA1-specific luminescent small molecules for the imaging and inhibition of latent EBV-infected tumor cells
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An EBNA1-specific small molecule (JLP2) has been synthesised. As a strong binder and dimerization inhibitor of EBNA1 in vitro, JLP2 may be used as a selective luminescent agent for the imaging and inhibition of latent EBV-infected ca
- Jiang, Lijun,Lui, Yin-Lai,Li, Hongguang,Chan, Chi-Fai,Lan, Rongfeng,Chan, Wai-Lun,Lau, Terrence Chi-Kong,Tsao, George Sai-Wah,Mak, Nak-Ki,Wong, Ka-Leung
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Read Online
- Organic nanoparticles of acetohydrazides as novel inhibitors for mild steel corrosion
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Novel organic nanoparticles (ONPs) of (E)-2-(4-(hydrazonomethyl)phenoxyl) acetohydrazide (H2) and N′((E)-benzylidene)-2-(4-((E)hydrazonomethyl)phenoxyl)acetohydrazide (H3) were prepared by the re-precipitation method. The ONPs were characterized using MS,
- Mandour, Howida S.,Nazeer, Ahmed Abdel,Al-Hetlani, Entesar,Madkour, Metwally,Abdel-Monem, Yasser K.
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Read Online
- PhotoTag: Photoactivatable Fluorophores for Protein Labeling
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We report experimental studies on the development of photoactivatable fluorophores for rapid, light-induced synthesis of protein conjugates. Proof-of-concept studies demonstrated that electronic excitation of photoactivatable BODIPY-ArN3 (1) in
- Fay, Rachael,Holland, Jason P.,Linden, Anthony
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Read Online
- Computational de novo design and characterization of a four-helix bundle protein that selectively binds a nonbiological cofactor
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We report the complete de novo design of a four-helix bundle protein that selectively binds the nonbiological DPP-Fe(III) metalloporphyrin cofactor (DPP-Fe(III) = 5, 15-Di[(4-carboxymethyleneoxy)phenyl]porphinato iron(III)). A tetrameric, D2-sy
- Cochran, Frank V.,Wu, Sophia P.,Wang, Wei,Nanda, Vikas,Saven, Jeffery G.,Therien, Michael J.,DeGrado, William F.
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Read Online
- Synthesis and antinociceptive profile of novel acidic sulphonylhydrazone derivatives from natural safrole
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The synthesis and antinociceptive activity of new sulphonylhydrazone derivatives is described. The synthetic route started from safrole, an abundant Brazilian natural product which occurs in sassafras oil (Ocotea pretiosa). The active compounds were obtai
- Lima, Lidia M.,Amarante, Emanuel G.,Miranda, Ana L.P.,Fraga, Carlos A.M.,Barreiro, Eliezer J.
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Read Online
- Photophysical and bactericidal properties of pyridinium and imidazolium porphyrins for photodynamic antimicrobial chemotherapy
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Despite advances achieved over the last decade, infections caused by multi-drug-resistant bacterial strains are increasingly becoming important societal issues that need to be addressed. New approaches have already been developed in order to overcome this problem. Photodynamic antimicrobial chemotherapy (PACT) could provide an alternative to fight infectious bacteria. Many studies have highlighted the value of cationic photosensitizers in order to improve this approach. This study reports the synthesis and the characterization of cationic porphyrins derived from methylimidazolium and phenylimidazolium porphyrins, along with a comparison of their photophysical properties with the well-known N-methylpyridyl (pyridinium) porphyrin family. PACT tests conducted with the tetracationic porphyrins of these three families showed that these new photosensitizers may offer a good alternative to the classical pyridinium porphyrins, especially against S.aureus and E.coli. In addition, they pave the way to new cationic photosensitizers by the means of derivatization through amide bond formation.
- Arnoux, Philippe,Frochot, Céline,Guern, Florent Le,Leroy-Lhez, Stéphanie,Nurlykyz, Yesmurzayeva,Ouk, Tan-Sothéa,Sol, Vincent,Yerzhan, Issabayev
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- Fluorescent multi-component polymer sensors for the sensitive and selective detection of Hg2+/Hg+ions: Via dual mode fluorescence and colorimetry
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Multi-component polymers (MCPs) incorporate multiple components into the main chain or pendant group and have special functions. In this work, the small-molecule fluorescent boron-dipyrromethene (BODIPY), with ester groups and/or alkoxyl long chains, was synthesized first. Then, this small-molecule BODIPY and the components containing CC bonds (HD and PD) were reacted via the Heck coupling reaction to obtain macromolecular probes that perform different functions. With the help of ester groups and alkoxyl "tail", polymers MCP1 and MCP2 were soluble in a variety of water-miscible organic solvents. Moreover, MCP3 and MCP4 were completely soluble in water. These macromolecular probes showed sensitive and selective recognition toward Hg2+/Hg+ because of the introduced components (HD and PD) containing CC bonds. After binding to Hg2+/Hg+, MCP1 and MCP2 demonstrated fluorescence quenching and color changes, which allowed the dual-channel specific detection of Hg2+/Hg+. Compared with the probes containing HD, the probes containing PD showed higher sensitivity, and the good recognition ability caused the detection limit to be as low as 0.32 μM, which may be due to the "molecular wire"mechanism. The small-molecule components with different functional groups were polymerized into fluorescent polymer materials. This methodology endows the polymer probe with good solubility and high sensitivity, and the as-prepared polymers could sense metal ions in aqueous environments. This journal is
- Cheng, Xinjian,Liu, Kaiqi,Marin, Luminita,Xiao, Li
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p. 22888 - 22901
(2021/12/24)
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- Microwave-assisted efficient synthesis of pyrazole-fibrate derivatives as stimulators of glucose uptake in skeletal muscle cells
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The design and synthesis of a series of pyrazolo[3,4-d]pyrimidinones containing fibrate side chains have been accomplished by utilizing the concept of molecular hybridization. All the synthesized compounds were evaluated for the glucose uptake stimulatory effect in L6 rat skeletal muscle cells. Four compounds (3f, 3g, 3j and 3q) were found to show significant stimulation of glucose uptake. Further these four compounds have been examined for their Glut4 translocation stimulatory effect in L6-Glut4myc myotubes. Compound 3q was found to exert maximum increase in GLUT4myc translocation.
- Gupta, Sampa,Kant, Ruchir,Pandey, Shubham,Rai, Amit Kumar,Sashidhara, Koneni V.,Singh, L. Ravithej,Tamrakar, Akhilesh K.
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supporting information
(2021/01/12)
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- Acylhydrazone derivative containing phosphonate and preparation method and application thereof
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The invention discloses an acylhydrazone derivative containing phosphonate and a preparation method and application thereof. The structural general formula of the acylhydrazone derivative containing phosphonate is as shown in the specification. According
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Paragraph 0024; 0026; 0027; 0028; 0029
(2020/03/12)
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- Preparation and evaluation of 99mTc-labeled porphyrin complexes prepared using PNP and HYNIC cores: Studying the effects of core selection on pharmacokinetics and tumor uptake in a mouse model
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Porphyrins are tetrapyrrolic macrocyclic ligands known for their affinity towards neoplastic tissues and once radiolabeled with a suitable diagnostic radioisotope could potentially be used for the imaging of tumorous lesions. In the present study, an unsy
- Guleria, Mohini,Das, Tapas,Vats, Kusum,Amirdhanayagam, Jeyachitra,Mathur, Anupam,Sarma, Haladhar D.,Dash, Ashutosh
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p. 606 - 615
(2019/04/30)
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- Micellar Br?nsted Acid Mediated Synthesis of DNA-Tagged Heterocycles
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The translation of well-established molecular biology methods such as genetic coding, selection, and DNA sequencing to combinatorial organic chemistry and compound identification has made extremely large compound collections, termed DNA-encoded libraries,
- ?kopi?, M. Klika,G?tte,Gramse,Dieter,Pospich,Raunser,Weberskirch,Brunschweiger
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supporting information
p. 10546 - 10555
(2019/07/04)
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- Chalcone aryloxyacetamide compound as well as preparation method and application thereof
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The invention relates to the field of pharmaceutical chemistry, in particular to a chalcone aryloxyacetamide compound (I) or (II) and a preparation method thereof. As proved by a pharmacodynamic test,the compound has the effects of reducing blood glucose, reducing triglyceride and reducing cholesterol, and can be used for treating abnormal glucolipid metabolism and obesity. A general formula of the compound is shown in the description.
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Paragraph 0031-0037
(2018/03/26)
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- Design, synthesis chalcone derivatives as AdipoR agonist for type 2 diabetes
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Two structurally novel series of chalcone derivatives were designed and synthesized as potential agents against type 2 diabetes. As a result of the antidiabetic biological evaluation in streptozotocin (STZ)-induced type 2 diabetes animal model, 13e, 13g, and 19f showed more significant reduction in serum Glu, TG, TC levels by contrast to the positive control AdipoRon. In addition to upregulating the expression of AdipoR1 and AdipoR2, 13e and 19f treatment also increased expression of AMPK and PPAR-α. Taken together, these results suggested that 13e and 19f might be a promising compound for type 2 diabetes treatment.
- Zhu, Panhu,Huang, Weijun,Li, Jiaming,Ma, Xiaodong,Hu, Mengqi,Wang, Yujun,Xu, Qinlong,Wang, Xianna
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p. 1525 - 1536
(2018/06/04)
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- Novel non-peptidic small molecule inhibitors of secreted aspartic protease 2 (SAP2) for the treatment of resistant fungal infections
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Targeting secreted aspartic protease 2 (SAP2), a kind of virulence factor, represents a new strategy for antifungal drug discovery. In this report, the first-generation of small molecule SAP2 inhibitors was rationally designed and optimized using a structure-based approach. In particular, inhibitor 23h was highly potent and selective and showed good antifungal potency for the treatment of resistant Candida albicans infections.
- Dong, Guoqiang,Liu, Yang,Wu, Ying,Tu, Jie,Chen, Shuqiang,Liu, Na,Sheng, Chunquan
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supporting information
p. 13535 - 13538
(2019/01/05)
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- Studies towards elucidating the potential of 5,10,15,20-tetrakis(: P -carboxy-methyleneoxyphenyl)porphyrin as a theranostic agent for applications in PET and PDT
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Porphyrins, owing to their inherent tendency to accumulate in tumorous lesions, are considered suitable for developing agents for theranostic applications involving tumor diagnosis and targeted tumor therapy. The aim of the present work is to study the po
- Guleria, Mohini,Kumar, Chandan,Das, Tapas,Amirdhanayagam, Jeyachitra,Sharma, Rohit,Sarma, Haladhar D.,Dash, Ashutosh
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p. 657 - 666
(2018/05/03)
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- COLORING COMPOSITION AND RECORDING METHOD
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PROBLEM TO BE SOLVED: To provide a coloring composition that can form an image having silver gloss. SOLUTION: A coloring composition contains a stilbene compound represented by general formula (1), and two or more solvents. For the two or more solvents, a
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Paragraph 0101
(2018/03/23)
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- COLORING COMPOSITION
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PROBLEM TO BE SOLVED: To provide a coloring composition capable of forming images having metallic gloss colors of various colors without precipitation of a luster coloring material. SOLUTION: A coloring composition includes a stilbene-based compound repre
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Paragraph 0073; 0074; 0095; 0096; 0100
(2018/05/24)
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- ORGANIC COLORANT HAVING SILVER GLOSS AND COLORING COMPOSITION
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PROBLEM TO BE SOLVED: To provide an organic colorant having a silver gloss. SOLUTION: An organic colorant having a silver gloss comprises a stilbene compound represented by the following formula. SELECTED DRAWING: None COPYRIGHT: (C)2017,JPOandINPIT
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Paragraph 0058
(2017/12/01)
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- Design, synthesis, and biological evaluation of chalcone- containing shikonin derivatives as inhibitors of tubulin polymerization
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The biological importance of microtubules in mitosis makes them an interesting target for the development of anticancer agents. In this study, a series of novel chalcone-containing shikonin derivatives was designed, synthesized, and evaluated for biologic
- Qiu, Han-Yue,Wang, Fang,Wang, Xue,Sun, Wen-Xue,Qi, Jin-Liang,Pang, Yan-Jun,Yang, Rong-Wu,Lu, Gui-Hua,Wang, Xiao-Ming,Yang, Yong-Hua
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p. 399 - 406
(2017/12/07)
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- Exploration of a Au(i)-mediated three-component reaction for the synthesis of DNA-tagged highly substituted spiroheterocycles
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We demonstrate a Au(i)-mediated three-component reaction to DNA-tagged highly substituted 6-oxa-1,2-diazaspiro[4.4]nonanes from either DNA-coupled aldehydes, hydrazides, or alkynols. The choice of the starting material coupled to the DNA tag was critial for the purity of the product as the DNA-aldehyde conjugate yielded the purest products, whereas the alkynol- and hydrazide conjugates returned complex product mixtures. The reaction was compatible with thymine-, cytosine-, and, surprisingly, with adenine-DNA, while guanine-containing DNA strands were degraded under the reaction conditions.
- Klika ?kopi?, Mateja,Willems, Suzanne,Wagner, Bernd,Schieven, Justin,Krause, Norbert,Brunschweiger, Andreas
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supporting information
p. 8648 - 8654
(2017/10/27)
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- Discovery of ONO-7300243 from a Novel Class of Lysophosphatidic Acid Receptor 1 Antagonists: From Hit to Lead
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Lysophosphatidic acid (LPA) evokes various physiological responses through a series of G protein-coupled receptors known as LPA1-6. A high throughput screen against LPA1 gave compound 7a as a hit. The subsequent optimization of 7a led to ONO-7300243 (17a) as a novel, potent LPA1 antagonist, which showed good efficacy in vivo. The oral dosing of 17a at 30 mg/kg led to reduced intraurethral pressure in rats. Notably, this compound was equal in potency to the α1 adrenoceptor antagonist tamsulosin, which is used in clinical practice to treat dysuria with benign prostatic hyperplasia (BPH). In contrast to tamsulosin, compound 17a had no impact on the mean blood pressure at this dose. These results suggest that LPA1 antagonists could be used to treat BPH without affecting the blood pressure. Herein, we report the hit-to-lead optimization of a unique series of LPA1 antagonists and their in vivo efficacy.
- Terakado, Masahiko,Suzuki, Hidehiro,Hashimura, Kazuya,Tanaka, Motoyuki,Ueda, Hideyuki,Kohno, Hiroshi,Fujimoto, Taku,Saga, Hiroshi,Nakade, Shinji,Habashita, Hiromu,Takaoka, Yoshikazu,Seko, Takuya
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supporting information
p. 913 - 918
(2016/10/22)
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- Bioinspired nanophotosensitizers: Synthesis and characterization of porphyrin-noble metal nanoparticle conjugates
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A methodology to enhance biological delivery of photosensitizers by incorporating them into nanomaterials has been developed. In order to prepare photosensitizer nanoconjugates as biocompatible and selective probes, initially, bioconjugatable porphyrinic
- Bhaumik, Jayeeta,Gogia, Gitanjali,Kirar, Seema,Vijay, Lekshmi,Thakur, Neeraj S.,Banerjee, Uttam C.,Laha, Joydev K.
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p. 724 - 731
(2016/01/12)
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- A process for the preparation of intermediates palestinian multi-past fragrance acetate
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The invention discloses a method for preparing a bazedoxifene acetate intermediate. The preparation method comprises the following steps: 1, condensing 4-hydroxybenzaldehyde S01 and alkylate S02 to prepare a 4-formyl phenoxy derivative M01; 2, performing
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Paragraph 0069-0072
(2017/01/31)
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- SIGMA-2 RECEPTOR LIGAND DRUG CONJUGATES AS ANTITUMOR COMPOUNDS, METHODS OF SYNTHESIS AND USES THEREOF
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Methods and compositions for treating cancers such as pancreatic cancer and synovial sarcoma are disclosed. Compounds comprising a sigma-2 receptor-binding moiety and a ferroptosis-inducing moiety are described. At least one described molecular species exhibits an IC50 value below 5 μΜ against human pancreatic cancer cells in vitro. Administration of this species promoted shrinkage of pancreatic cancer tumors in a murine model system in vivo, and led to 100% survival of experimental animals over a time course in which control therapies provided only 30% or 40% survival. Methods of synthesis of molecular species are also disclosed.
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Paragraph 0158
(2016/01/29)
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- Targeting quorum sensing by designing azoline derivatives to inhibit the N-hexanoyl homoserine lactone-receptor CviR: Synthesis as well as biological and theoretical evaluations
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To counteract bacterial resistance, we investigated the interruption of quorum sensing mediated by non-classical bioisosteres of the N-hexanoyl homoserine lactone with an azoline core. For this purpose, a set of selected 2-substituted azolines was synthesized, establishing the basis for a new protocol to synthesize 2-amino imidazolines. The synthesized compounds were evaluated as inhibitors of violacein production in Chromobacterium violaceum. Theoretical studies on bioisostere-protein interactions were performed using CviR. The results show that some azolines decreased violacein production, suggesting an antiquorum sensing profile against Gram-negative bacteria. Docking and molecular dynamic simulations together with binding free energy calculations revealed the exact binding and inhibitory profiles. These theoretical results show relationship with the in vitro activity of the azoline series.
- Bucio-Cano, Alejandro,Reyes-Arellano, Alicia,Correa-Basurto, José,Bello, Martiniano,Torres-Jaramillo, Jenifer,Salgado-Zamora, Héctor,Curiel-Quesada, Everardo,Peralta-Cruz, Javier,Avila-Sorrosa, Alcives
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p. 7565 - 7577
(2015/12/18)
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- Discovery of Thiazolidine-2,4-Dione/Biphenylcarbonitrile Hybrid as Dual PPAR α/γ Modulator with Antidiabetic Effect: In vitro, In Silico and In Vivo Approaches
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A small series of thiazolidine-2,4-dione and barbituric acid derivatives 1-4 was prepared using a short synthetic route, and all compounds were characterized by elemental analysis, mass spectrometry, and NMR (1H, 13C) spectroscopy. T
- Hidalgo-Figueroa, Sergio,Ramirez-Espinosa, Juan J.,Estrada-Soto, Samuel,Almanza-Perez, Julio C.,Roman-Ramos, Ruben,Alarcon-Aguilar, Francisco J.,Hernandez-Rosado, Jesus V.,Moreno-Diaz, Hermenegilda,Diaz-Coutino, Daniel,Navarrete-Vazquez, Gabriel
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p. 474 - 483
(2013/05/21)
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- IMIDAZO [4, 5 - B] PYRIDINE DERIVATIVES AS ALK AND JAK MODULATORS FOR THE TREATMENT OF PROLIFERATIVE DISORDERS
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This application relates to compounds of the Formula I as defined herein, and/or salts thereof. This application further relates to compositions and methods of using these compounds and/or salts thereof. The compounds of Formula I are useful as ALK and JAK modulators for the treatment of proliferative disorders.
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Page/Page column 224; 226
(2013/08/15)
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- Indole-based fibrates as potential hypolipidemic and antiobesity agents
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Hypolipidemic and antiobesity effects of the newly synthesized indole-based fibrates were evaluated in Triton WR-1339 and high fat diet (HFD)-induced hyperlipidemic rats. Preliminary screening of all the synthesized compounds was done by using an acute model (Triton model), in which compounds 3f and 3l showed significant antidyslipidemic activity. Furthermore, these compounds 3f and 3l were found to induce significant weight loss in the visceral fat mass of HFD-fed hyperlipidemic rats without affecting the normal feeding behavior. Histological examination of the liver of rats supplemented with 3f and 3l revealed a significant decrease in steatosis when compared to the effect of the standard drug fenofibrate. Additional effects such as an increase in lecithin cholesterol acyl-transferase (LCAT) enzyme level and increased receptor mediated catabolism of I131-low density lipoproteins (LDL) confirm and reinforce the efficacy of both of these compounds as a new class of dual-acting hypolipidemic and antiobesity agents.
- Sashidhara, Koneni V.,Kumar, Manoj,Sonkar, Ravi,Singh, Bhanu Shankar,Khanna,Bhatia, Gitika
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experimental part
p. 2769 - 2779
(2012/06/04)
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- Potash alum [KAL(SO4)2.12H2O] catalysed esterification of formylphenoxyaliphatic acids
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A convenient and clean procedure for esterification is reported. Direct condensation of formylphenoxyaliphatic acids with low to high boiling alcohols catalysed by potash alum gave moderate to good yields. This catalyst could be recovered and reused without substantial loss in its catalytic activity and the methodology could be used for a range of closely related substrates.
- Shunmugadhas, Ganesan,Kumar, Suresh,Kumaresan, Sudalaiandi
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p. 857 - 863,7
(2020/09/09)
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- A class of 5-benzylidene-2-phenylthiazolinones with high potency as direct 5-lipoxygenase inhibitors
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A novel class of potent direct 5-lipoxygenase (5-LO) inhibitors bearing a thiazolinone-scaffold identified by virtual screening is presented. A range of substitutions and the importance of the 2-phenyl moiety were evaluated. This series is characterized by high potency in intact polymorphonuclear leukocytes and a cell-free system, exemplified by (Z)-2-(4-chlorophenyl)-5-(4- methoxybenzylidene)-5H-thiazol-4-one (18, IC50 = 0.28 and 0.09 μ-M). These disubstituted thiazolinones may possess potential for intervention with inflammatory and allergic diseases and certain cancer types.
- Hofmann, Bettina,Barzen, Sebastian,R?dl, Carmen B.,Kiehl, Andreas,Borig, Julia,?ivkovi-, Aleksandra,Stark, Holger,Schneider, Gisbert,Steinhilber, Dieter
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supporting information; experimental part
p. 1943 - 1947
(2011/05/14)
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- A green chemistry method for the regeneration of carbonyl compounds from oximes by using cupric chloride dihydrate as a recoverable promoter for hydrolysis
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A mild, efficient, general, and green method for the regeneration of carbonyl compounds from their corresponding oximes is described. Cupric salts promoted hydrolysis of oximes was studied, and the best reaction conditions for the hydrolysis have been found. Carbonyl compounds were obtained in 85-98% yields after the treatment of oximes with 2 molar equivalent of CuCl 22H2O at reflux (around 75 C) in a mixed solvent of acetonitrile and water (4:1). In addition, cupric salt was readily recovered in an almost quantitative yield via the complete precipitation of Cu(OH) 22H2O. Georg Thieme Verlag Stuttgart · New York.
- Quan, Na,Shi, Xiao-Xin,Nie, Liang-Deng,Dong, Jing,Zhu, Rui-Heng
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experimental part
p. 1028 - 1032
(2011/06/17)
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- Novel Compounds
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The present invention provides compounds of formula (I): wherein Ra, Rb, Rc, R1, R2, R3, X1, Y1, Z1, A, n and m are as defined in the specification, and pharmaceutically acceptable salts thereof, as well as processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
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Page/Page column 67
(2011/06/24)
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- Synthesis of meso-tetraarylporphyrins possessing amino and carboxy groups and their peptides
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meso-Tris(3,5-di-tert-butylphenyl)porphyrin (P-H) is bonded with L-phenylalanine (H-Phe-OH) directly at the unsubstituted meso-position of the former and the p-position of phenyl group of the latter to afford chiral porphyrin-amino acid conjugate H-Phe(p-
- Tamiaki, Hitoshi,Kozawa, Takaaki,Kitamoto, Rika,Kunieda, Michio
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experimental part
p. 375 - 388
(2010/11/19)
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- RADIATION-SENSITIVE COMPOSITION
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A radiation-sensitive composition containing a resist compound having a high sensitivity, a high resolution, a high etching resistance, and a low outgas which forms a resist pattern with a good shape is described. Further described is a method of forming a resist pattern using the radiation-sensitive composition. Still further described are a novel composition for forming a photoresist under coat film which is excellent in optical properties and etching resistance and contains substantially no sublimable substance and an under coat film formed by the composition. Still further described are a radiation-sensitive composition containing a solvent and a cyclic compound having a specific structure, for example, a cyclic compound (A) having a molecular weight of 700 to 5000 which is synthesized by the condensation reaction of a compound having 2 to 59 carbon atoms and 1 to 4 formyl groups (aldehyde compound (A1)) with a compound having 6 to 15 carbon atoms and 1 to 3 phenolic hydroxyl groups (phenol compound (A2)), and a cyclic compound for use in the radiation-sensitive composition.
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Page/Page column 112
(2009/08/14)
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- Masked imidazolyl-dipyrromethanes in the synthesis of imidazole-substituted porphyrins
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Imidazole-substituted metalloporphyrins are valuable for studies of self-assembly and for applications where water solubility is required. Rational syntheses of porphyrins bearing one or two imidazol-2-yl or imidazol-4-yl groups at the meso positions have been developed. The syntheses employ dipyrromethanes, 1-acyldipyrromethanes, and 1,9-diacyldipyrromethanes bearing an imidazole group at the 5-position. The polar, reactive imidazole unit was successfully masked by use of (1) the 2-(trimethylsilyl)ethoxymethyl (SEM) group at the imidazole pyrrolic nitrogen, and (2) a dialkylboron motif bound to the pyrrole of the dipyrromethane and coordinated to the imidazole imino nitrogen. The nonpolar nature of such doubly masked imidazolyl-dipyrromethanes facilitated handling. Selected masked dipyrromethanes were characterized by 11B and 15N NMR spectroscopy. Five distinct methods were examined to obtain trans-A2B2-, trans-AB2C-, and trans-AB-porphyrins. Each porphyrin contained one or two SEM-protected imidazole units. The SEM group could be removed with TBAF or HCl. Two zinc(II) porphyrins and a palladium(II) porphyrin bearing a single imidazole moiety were prepared and subjected to alkylation (with ethyl iodide, 1,3-propane sultone, or 1,4-butane sultone) to give water-soluble imidazolium-porphyrins. This work establishes the foundation for the rational synthesis of a variety of porphyrins containing imidazole units.
- Bhaumik, Jayeeta,Yao, Zhen,Borbas, K. Eszter,Taniguchi, Masahiko,Lindsey, Jonathan S.
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p. 8807 - 8817
(2007/10/03)
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- Ethyne-bridged (porphinato)zinc(II)-(porphinato)iron(III) complexes: Phenomenological dependence of excited-state dynamics upon (porphinato)iron electronic structure
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We report the synthesis, spectroscopy, potentiometric properties, and excited-state dynamical studies of 5-[(10,20-di-((4-ethyl ester)methylene-oxy) phenyl)porphinato]zinc(II)-[5′-[(10′,20′- di-((4-ethyl ester)methylene-oxy)phenyl)porphinato]iron(III)-chl
- Duncan, Timothy V.,Wu, Sophia P.,Therien, Michael J.
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p. 10423 - 10435
(2007/10/03)
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- A stable single piece of unimolecularly π-stacked porphyrin aggregate in a thixotropic low molecular weight gel: A one-dimensional molecular template for polydiacetylene wiring up to several tens of micrometers in length
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An amide-type copper porphyrin gelator having alkyldiacetylene tethers gives very transparent gel in Decalin, and the gel shows unique thixotropic behavior. One-dimensional aggregates generated in the gel act as templates for unimolecularly segregated pol
- Shirakawa, Michihiro,Fujita, Norifumi,Shinkai, Seiji
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p. 4164 - 4165
(2007/10/03)
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- Imidazo[2,1-b]thiazepines: Synthesis, structure and evaluation of benzodiazepine receptor binding
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As a continuation of our search for new ligands acting on benzodiazepine receptors among the fused 2-thiohydantoin derivatives, a series of 5-substituted imidazo[2,1-b]thiazepines was synthesized and investigated in radioligand binding studies at the benz
- Kiec-Kononowicz, Katarzyna,Karolak-Wojciechowska, Janina,Michalak, Barbara,Pekala, Elzbieta,Schumacher, Britta,Mueller, Christa E.
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p. 205 - 218
(2007/10/03)
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- TARGET-ORIENTED CHEMOTHERAPY FOR TREATING TUMORS OF THE SEXUAL ORGANS
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The invention relates to dialkyltriazene-supporting estrogens and antiestrogens that are suited for use as chemotherapeutic drugs for treating carcinomas of the sexual organs of humans and animals.
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Page/Page column 29
(2010/02/09)
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- Lignin Peroxidase-Catalyzed Oxidation of Nonphenolic Trimeric Lignin Model Compounds: Fragmentation Reactions in the Intermediate Radical Cations
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The H2O2-promoted oxidations of the two nonphenolic β-O-aryl lignin model trimers 1 and 2, catalyzed by lignin peroxidase (LiP) at pH = 3.5, have been studied. The results have been compared with those obtained in the oxidation of 1 and 2 with the genuine one-electron oxidant potassium 12-tungstocobalt(III)ate. These models present a different substitution pattern of the three aromatic rings, and by one-electron oxidation, they form radical cations with the positive charge, which is localized in the dialkoxylated ring as also evidenced by a pulse radiolysis study. Both the oxidations with the enzymatic and with the chemical systems lead to the formation of products deriving from the cleavage of C-C and C-H bonds in a β position with respect to the radical cation with the charge residing in the dialkoxylated ring (3,4-dimethoxybenzaldehyde (5) and a trimeric ketone 6 in the oxidation of 1 and a dimeric aldehyde 8 and a trimeric ketone 9 in the oxidation of 2). These products are accompanied by a dimeric aldehyde 7 in the oxidation of 1 and 4-methoxybenzaldehyde (10) in the oxidation of 2. The unexpected formation of these two products has been explained by suggesting that 1.+ and 2.+ can also undergo an intramolecular electron transfer leading to the radical cations 1a.- and 2a .+ with the charge residing in a monoalkoxylated ring. The fast cleavage of a C-C bond β to this ring, leading to 7 from 1.+ and to 10 from 2.+, is the driving force of the endoergonic electron transfer. A kinetic steady-state investigation of the LiP-catalyzed oxidation of the trimer 2, the dimeric model 1-(3,4-dimethoxyphenyl)-2-phenoxy-1-ethanol (4), and 3,4-dimethoxybenzyl alcohol (3) has indicated that the turnover number (kcat) and the affinity for the enzyme decrease significantly by increasing the size of the model compound. In contrast, the three substrates exhibited a very similar reactivity toward a chemical oxidant [Co IIIW]. This suggests a size-dependent interaction of the enzyme with the substrate which may influence the efficiency of the electron transfer.
- Baciocchi, Enrico,Fabbri, Claudia,Lanzalunga, Osvaldo
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p. 9061 - 9069
(2007/10/03)
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- Process for the preparation of thiazolidine-2,4-dione derivatives
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An improved process for the preparation of 5-[4-[[3-Methyl-4-oxo-3,4-dihydroquinazolin-2-yl]methoxy]benzyl]thiazolidine-2,4-dione of formula (1) which comprises: reducing the compound of formula (2′) where R represents a (C1-C4)alkyl
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- Pyridopyrimidones, quinolines and fused N-heterocycles as bradykinin antagonists
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This invention relates to a compound of the formula: STR1 wherein Z is a group of the formula: STR2 in which X1 is N or C--R1, X2 is N or C--R9, X3 is N or C--R2, R1 is lower alk
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- N-(3-pyridylalkyl)sulfonamide compounds which have useful pharmaceutical activity
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Illustrative examples of the N-(3-pyridylalkyl)sulfonamide derivative are represented by the following formulae [II] and [III]: STR1 The derivatives are available for a thromboxane A2 production inhibitor, a thromboxane A2 antagonist, a prostaglandin H2 antagonist, an anti-thrombus agent, a thrombus-preventing agent and an anti-allergy agent.
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- SYNTHESIS OF TETRAPHENYLPORPHINES WITH ACTIVE GROUPS IN THE PHENYL RINGS. 5. TETRA(CARBOXYMETHYLENOXYPHENYL)PORPHINES AND THEIR ETHYL ESTERS.
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Tetra(carboxymethylenoxyphenyl)porphines which are soluble in bases are prepared by hydrolysis of the ethyl esters of tetra(carboxymethylenoxyphenyl)porphines.The starting ethyl esters of the tetra(carboxymethylenoxyphenyl)porphines were synthesized by alkylation of tetra(oxyphenyl)porphines with ethylchloroacetate, as well as by condensation of pyrrole with ethyl esters of formylphenoxyacetic acids.
- Syrbu, S. A.,Semeikin, A. S.,Berezin, B. D.,Koifman, O. I.
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p. 1149 - 1153
(2007/10/02)
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- Synthesis of Some Newer 4-(3-Methyl-5-oxo-4-pyrazolidenemethyl)phenoxyacetic Acid Benzylidenehydrazides and &α-Methylbenzylidenehydrazides as CNS Active and Antiinflammatory Agents
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The title compounds (IVa-q) have been synthesized and found to be non-toxic and CNS depressant or stimulant.In antiinflammatory activity, these compounds show 4-23percent protection against the carrageenin-induced mice paw oedema.
- Mohan, Rajiv Ravindra,Agarwal, Chapla,Misra, V. S.
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p. 339 - 341
(2007/10/02)
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