- Myricetin derivative containing sulfonyl piperazine as well as preparation method and application thereof
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The invention discloses a myricetin derivative containing sulfonyl piperazine as well as a preparation method and application of the myricetin derivative. The structural general formula of the myricetin derivative is shown in the specification, and n is t
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Paragraph 0029; 0035-0036
(2021/01/24)
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- Synthesis and antibacterial activity of novel myricetin derivatives containing sulfonylpiperazine
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Myricetin derivatives containing sulfonylpiperazine were synthesized and their structures were confirmed by NMR and HRMS. The antibacterial activity results indicated that some compounds showed good antibacterial activity against Xanthomonas oryzaepv. ory
- He, Jun,Tang, Xue-Mei,Liu, Ting-Ting,Peng, Feng,Zhou, Qing,Liu, Li-Wei,He, Ming,Xue, Wei
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p. 1021 - 1027
(2020/10/02)
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- Discovery of Novel Chromone Derivatives Containing a Sulfonamide Moiety as Anti-ToCV Agents through the Tomato Chlorosis Virus Coat Protein-Oriented Screening Method
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A number of novel chromone derivatives containing sulfonamide moieties were designed and synthesized, and the activity of compounds against tomato chlorosis virus (ToCV) was assessed using the ToCVCP-oriented screening method. Comparative molecular field analysis (CoMFA) and comparative molecular similarity index analysis (CoMSIA) models were established based on the dissociation constant (Kd) values of the target compounds, and compound 35 was designed and synthesized with the aid of CoMFA and CoMSIA models. The study of affinity interaction indicated that compound 35 exhibited excellent affinity with ToCVCP with a Kd value of 0.11 μM, which was better than that of the positive control agents xiangcaoliusuobingmi (0.44 μM) and ningnanmycin (0.79 μM). In addition, the in vivo inhibitory effect of compound 35 on the ToCVCP gene was evaluated by the quantitative real-time polymerase chain reaction. ToCVCP gene expression levels of the compound 35 treatment group were reduced by 67.2%, which was better than that of the positive control agent ningnanmycin (59.5%). Therefore, compound 35 can be used as a potential anti-ToCV drug in the future.
- Jiang, Donghao,Chen, Jixiang,Zan, Ningning,Li, Chunyi,Hu, Deyu,Song, Baoan
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p. 12126 - 12134
(2021/10/26)
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- Design and synthesis of substituted (1-(benzyl)-1: H -1,2,3-triazol-4-yl)(piperazin-1-yl)methanone conjugates: Study on their apoptosis inducing ability and tubulin polymerization inhibition
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A library of substituted (1-(benzyl)-1H-1,2,3-triazol-4-yl)(piperazin-1-yl)methanone derivatives were designed, synthesized and screened for their in vitro cytotoxic activity against BT-474, HeLa, MCF-7, NCI-H460 and HaCaT cells by employing 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Among all the synthesized analogues, compound 10ec displayed the highest cytotoxicity with the IC50 value of 0.99 ± 0.01 μM towards BT-474 cancer cell line. The target compound (10ec) was also evaluated for its tubulin polymerization inhibition study. Detailed biological studies such as acridine orange/ethidium bromide (AO/EB), DAPI and annexin V-FITC/propidium iodide staining assay suggested that compound 10ec induced the apoptosis of BT-474 cells. The clonogenic assay revealed that the inhibition of colony formation in BT-474 cells by 10ec in concentration-dependent manner. Moreover, the flow cytometric analysis revealed that 10ec induced apoptosis via cell cycle arrest at the sub-G1 and G2/M phase. In silico studies of sulfonyl piperazine-integrated triazole conjugates unveil that they possess drug-like properties. According to the molecular modelling studies, compound 10ec binds to the colchicine binding site of the tubulin.
- Alvala, Mallika,Babu, Bathini Nagendra,Devi, Ganthala Parimala,Godugu, Chandraiah,Manasa, Kesari Lakshmi,Nagesh, Narayana,Sigalapalli, Dilep Kumar,Thatikonda, Sowjanya,Vuppaladadium, Sowmya
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supporting information
p. 1295 - 1302
(2020/12/01)
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- Rational modifications, synthesis and biological evaluation of new potential antivirals for RSV designed to target the M2-1 protein
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Respiratory syncytial virus (RSV) is the main cause of lower respiratory tract diseases in infants and young children, with potentially serious and fatal consequences associated with severe infections. Despite extensive research efforts invested in the identification of therapeutic measures, no vaccine is currently available, while treatment options are limited to ribavirin and palivizumab, which both present significant limitations. While clinical and pre-clinical candidates mainly target the viral fusion protein, the nucleocapsid protein or the viral polymerase, our focus has been the identification of new antiviral compounds targeting the viral M2-1 protein, thanks to the presence of a zinc-ejecting group in their chemical structure. Starting from an anti-RSV hit we had previously identified with an in silico structure-based approach, we have designed, synthesised and evaluated a new series of dithiocarbamate analogues, with which we have explored the antiviral activity of this scaffold. The findings presented in this work may provide the basis for the identification of a new antiviral lead to treat RSV infections.
- Bassetto, Marcella,Benato, Sara,Brancale, Andrea,Ferla, Salvatore,Jochmans, Dirk,Manganaro, Roberto,Neyts, Johan,Paulissen, Jasmine
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supporting information
(2020/03/13)
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- Synthesis and biological evaluation of imidazo[2,1-b]thiazole based sulfonyl piperazines as novel carbonic anhydrase ii inhibitors
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A novel series of imidazo[2,1-b]thiazole-sulfonyl piperazine conjugates (9aa-ee) has been synthesized and evaluated for carbonic anhydrase (CA, EC 4.2.1.1) inhibitory potency against four isoforms: The cytosolic isozyme hCA I, II and trans-membrane tumor-
- Alvala, Mallika,Angeli, Andrea,Manasa, Kesari Lakshmi,Mohammed, Arifuddin,Pujitha, Sravya,Sethi, Aaftaab,Supuran, Claudiu T.
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- Design and synthesis of β-carboline linked aryl sulfonyl piperazine derivatives: DNA topoisomerase II inhibition with DNA binding and apoptosis inducing ability
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A series of new β-carboline linked aryl sulfonyl piperazine congeners have been synthesized by coupling various β-carboline acids with substituted aryl sulfonyl piperazines. Evaluation of their anticancer activity against a panel of human cancer cell lines such as colon (HT-29), breast (MDA-MB-231), bone osteosarcoma (MG-63), brain (U87 MG), prostate (PC- 3) and normal monkey kidney (Vero) cell line has been done. Among the series, compound 8ec and 8ed has shown most potent cytotoxicity with an IC50 values of 2.80 ± 0.10 μM and 0.59 ± 0.28 μM respectively against MG-63 cell line and also potent on other cell lines tested. Compounds 8ec and 8ed was found to inhibit Topo II that is confirmed by specific Topo II inhibition assay. DNA binding studies, cell cycle analysis, Annexin V study indicate that these compounds has potential anticancer activity. Molecular docking studies for compound 8ec and 8ed are incorporated to understand the nature of interaction with topoisomerase IIα and dsDNA.
- Alvala, Mallika,Godugu, Chandraiah,Kalle, Arunasree M.,Kiranmai, Gaddam,Lakshmi Manasa, Kesari,Nagendra Babu, Bathini,Nagesh, Narayana,Sagar, Arpita,Sigalapalli, Dilep Kumar,Thatikonda, Sowjanya
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- 9-piperazine sulfonamide-10-hydroxycamptothecine compound as well as preparation method and anti-tumor application thereof
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The invention relates to a novel 9-piperazine sulfonamide-10-hydroxycamptothecine compound shown as a formula (I), a preparation method of the compound and application of the compound in preparation of antitumor drugs. The chemical general formula of the
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Paragraph 0017; 0019-0022
(2020/10/06)
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- Synthesis of Novel Benzamide- piperazine-sulfonamide Hybrids as Potential Anticancer Agents
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The synthesis of a series of substituted hippuric acid (2-benzamidoacetic acid) derivatives containing arylsulfonylpiperazine nucleus (3a–j, 4a–j) is described. The compounds were synthesized by coupling hippuric/4-fluorohippuric acid with various arylsulfonylpiperazines using N-(3-dimethylaminopropyl)-N-ethylcarbodiimide (EDCI). The structures of all the new compounds were confirmed by IR, NMR and MS spectral data. All the synthesized compounds have been evaluated for their in vitro cytotoxicity towards five human cancer cell lines of different origins viz. HeLa (Cervical), A549 (Lung), A375 (Skin), MD-AMB-231(Breast) and T98G (brain) and their IC50 values were determined. Among the compounds tested, 3b, 3d, 3g, 4c and 4e displayed significant cytotoxic activity (IC50 = 24.2–38.2 μM). T98G was the most sensitive cell line towards the compounds studied followed by HeLa, A375, A549 and MD-AMB-231.
- Ramalingeswara Rao,Mohana Rao Katiki,Dileep Kommula,SaiShyam Narayanan,Ruby John Anto,Murty
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p. 393 - 402
(2019/12/12)
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- Sulfonylpiperazines based on a flavone as antioxidant and cytotoxic agents
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Chrysin-based sulfonylpiperazines 7a-k were synthesized and investigated for their in vitro free radical scavenging potential as well as cytotoxic efficacies against selected cancer cell lines. Cytotoxicity of the new compounds toward noncancer cells was
- Patel, Rahul V.,Mistry, Bhupendra M.,Syed, Riyaz,Parekh, Nikhil M.,Shin, Han-Seung
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- Development of 2-amino-4-phenylthiazole analogues to disrupt myeloid differentiation factor 88 and prevent inflammatory responses in acute lung injury
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Myeloid differentiation primary response protein 88 (MyD88), an essential adapter protein used by toll-like receptors (TLR), is a promising target molecule for the treatment of respiratory inflammatory diseases. Previous studies explored the activities of novel 2-amino-4-phenylthiazole analogue (6) in inflammation-induced cancer, and identified the analogue as an inhibitor of MyD88 toll/interleukin-1 receptor (TIR) homology domain dimerization. Here, we describe the synthesis of 47 new analogues by modifying different sites on this lead compound and assessed their anti-inflammatory activities in lipopolysaccharide-induced mouse primary peritoneal macrophages (MPMs). The most promising compound, 15d, was found to effectively interact with MyD88 protein and prevented formation of the MyD88 homodimeric complex. Furthermore, 15d showed in vivo anti-inflammatory activity in LPS-caused model of acute lung injury. This work provides new candidates as MyD88 inhibitors to combat inflammation diseases.
- Chen, Lingfeng,Chen, Hongjin,Chen, Pengqin,Zhang, Wenxin,Wu, Chao,Sun, Chuchu,Luo, Wu,Zheng, Lulu,Liu, Zhiguo,Liang, Guang
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- Development of novel chromeno[4,3-c]pyrazol-4(2H)-one derivates bearing sulfonylpiperazine as antitumor inhibitors targeting PI3Kα
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PI3K signal pathway plays a vital role in cellular functions and becomes an attractive approach for cancer therapy. Herein, a new series of novel chromeno[4,3-c]pyrazol-4(2H)-one derivatives bearing sulfonylpiperazine based on the PI3K inhibitors and our previous research. They were screened for their PI3K inhibitory activities and anticancer effects in vitro. Biological studies indicated that compound 7m revealed the remarkable antiproliferative activity (IC50 ranging from 0.03 to 0.09 μM) against four cancer cell lines (A549, Huh7, HL60 and HCT-116). Besides, compound 7m displayed a certain selective for PI3Kα (IC50 = 0.009 μM) over PI3Kβ, γ and δ, and meanwhile, it can remarkable decreased the expression level of p-Akt (Ser473) and p-S6K. In addition, compound 7m could not only induce HCT-116 cell arrest at G1 phase in a dose-dependent manner, but also induce cell apoptosis via upregulation of Bax and cleaved-caspase 3/9, and downregulation of Bcl-2. Besides, compound 7m can remarkably inhibit the growth of tumor in vivo. The above results suggested that compound 7m could be considered as a promising PI3Kα inhibitor.
- Yin, Yong,Sha, Shao,Wu, Xun,Wang, She-Feng,Qiao, Fang,Song, Zhong-Cheng,Zhu, Hai-Liang
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- Synthesis of Combretastatin-A4 Carboxamidest that Mimic Sulfonyl Piperazines by a Molecular Hybridization Approach: in vitro Cytotoxicity Evaluation and Inhibition of Tubulin Polymerization
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Molecular hybridization approach is a promising structural modification tool to design new chemical entities (NCEs) by mimicking two different pharmacophoric units into one scaffold to enhance the biological properties. With this aim, combretastatin-A4 ac
- Jadala, Chetna,Sathish, Manda,Anchi, Pratibha,Tokala, Ramya,Lakshmi, Uppu Jaya,Reddy, Velma Ganga,Shankaraiah, Nagula,Godugu, Chandraiah,Kamal, Ahmed
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supporting information
p. 2052 - 2060
(2019/11/22)
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- Hypervalent Iodine Mediated Sulfonamide Synthesis
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A new metal-free sulfonylation reaction is described. The method takes advantage of the Umpolung reactivity and group-transfer properties of iodine(III) compounds, combining hypervalent iodine reagents and sulfinate salts to deliver a clean and mild transfer of sulfonyl groups to amines and anilines. A total of 25 sulfonamides was synthesised in up to 99 % yield, even on gram-scale. The reaction mechanism was investigated by ESI-MS and DFT calculations.
- Poeira, Diogo L.,Macara, Jo?o,Faustino, Hélio,Coelho, Jaime A. S.,Gois, Pedro M. P.,Marques, M. Manuel B.
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supporting information
p. 2695 - 2701
(2019/04/08)
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- Structure-Activity Relationships of Potent, Targeted Covalent Inhibitors That Abolish Both the Transamidation and GTP Binding Activities of Human Tissue Transglutaminase
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Human tissue transglutaminase (hTG2) is a multifunctional enzyme. It is primarily known for its calcium-dependent transamidation activity that leads to formation of an isopeptide bond between glutamine and lysine residues found on the surface of proteins, but it is also a GTP binding protein. Overexpression and unregulated hTG2 activity have been associated with numerous human diseases, including cancer stem cell survival and metastatic phenotype. Herein, we present a series of targeted covalent inhibitors (TCIs) based on our previously reported Cbz-Lys scaffold. From this structure-activity relationship (SAR) study, novel irreversible inhibitors were identified that block the transamidation activity of hTG2 and allosterically abolish its GTP binding ability with a high degree of selectivity and efficiency (kinact/KI > 105 M-1 min-1). One optimized inhibitor (VA4) was also shown to inhibit epidermal cancer stem cell invasion with an EC50 of 3.9 μM, representing a significant improvement over our previously reported "hit" NC9.
- Akbar, Abdullah,McNeil, Nicole M. R.,Albert, Marie R.,Ta, Viviane,Adhikary, Gautam,Bourgeois, Karine,Eckert, Richard L.,Keillor, Jeffrey W.
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supporting information
p. 7910 - 7927
(2017/10/06)
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- Synthesis and biological evaluation of novel indole derivatives containing sulfonamide scaffold as potential tubulin inhibitor
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Microtubule-targeted drugs play a critical role in various types of cancer therapy worldwide. In our study, a series of novel indole derivatives containing a sulfonamide scaffold were designed, synthesized and biologically evaluated as potential tubulin p
- Man, Ruo-Jun,Tang, Dan-Jie,Lu, Xiao-Yuan,Duan, Yong-Tao,Tao, Xiang-Xiang,Yang, Meng-Ru,Wang, Le-Le,Wang, Bao-Zhong,Xu, Chen,Zhu, Hai-Liang
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supporting information
p. 1759 - 1767
(2016/09/23)
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- Expanding the scope of silane-mediated hydrodehalogenation reactions
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A palladium-catalysed, silane-mediated hydrodehalogenation (HDH) reaction with increased substrate scope has been developed. Whereas previous attempts to reduce carboxylic acid or phenol-containing aryl halides using silane-based HDH conditions failed, the current protocol allows efficient access to the reduced products. Chemoselective HDH in the presence of sensitive functional groups is also presented.
- Noonan, Gary M.,Hayter, Barry R.,Campbell, Andrew D.,Gorman, Timothy W.,Partridge, Benjamin E.,Lamont, Gill M.
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p. 4518 - 4521
(2013/08/23)
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- Structure-activity relationship studies of sulfonylpiperazine analogues as novel negative allosteric modulators of human neuronal nicotinic receptors
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Neuronal nicotinic receptors have been implicated in several diseases and disorders such as autism, Alzheimer's disease, Parkinson's disease, epilepsy, and various forms of addiction. To understand the role of nicotinic receptors in these conditions, it would be beneficial to have selective molecules that target specific nicotinic receptors in vitro and in vivo. Our laboratory has previously identified novel negative allosteric modulators of human α4β2 (Hα4β2) and human α3β4 (Hα3β4) nicotinic receptors. The effects of novel sulfonylpiperazine analogues that act as negative allosteric modulators on both Hα4β2 nAChRs and Hα3β4 nAChRs were investigated. This work, through structure-activity relationship (SAR) studies, describes the chemical features of these molecules that are important for both potency and selectivity on Hα4β2 nAChRs. (Figure presented)
- Henderson, Brandon J.,Carper, Daniel J.,González-Cestari, Tatiana F.,Yi, Bitna,Mahasenan, Kiran,Pavlovicz, Ryan E.,Dalefield, Martin L.,Coleman, Robert S.,Li, Chenglong,McKay, Dennis B.
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supporting information; experimental part
p. 8681 - 8692
(2012/02/15)
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- Novel benzo[ b ]thiophene derivatives as new potential antidepressants with rapid onset of action
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We report benzo[b]thiophene derivatives synthesized according to a dual strategy. 8j, 9c, and 9e with affinity values toward 5-HT7R and 5-HTT were selected to probe their antidepressant activity in vivo using the forced swimming text (FST). The results showed significant antidepressant activity after chronic treatment. 9c was effective in reducing the immobility time in FST even after acute treatment. These findings identify these compounds as a new class of antidepressants with a rapid onset of action.
- Berrade, Luis,Aisa, Bárbara,Ramirez, María J.,Galiano, Silvia,Guccione, Salvatore,Moltzau, Lise Román,Levy, Finn Olav,Nicoletti, Ferdinando,Battaglia, Giuseppe,Molinaro, Gemma,Aldana, Ignacio,Monge, Antonio,Perez-Silanes, Silvia
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supporting information; experimental part
p. 3086 - 3090
(2011/07/07)
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- Selective deprotection of methanesulfonamides to amines
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"Chemical Equation Presented" Methanesulfonamldes were deprotected to their parent amines via deprotonation and oxygenation with O 2 (g), even in the presence of other traditional sulfonamides.
- Naito, Hiroyuki,Hata, Takeshi,Urabe, Hirokazu
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experimental part
p. 1228 - 1230
(2010/06/13)
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- ISOTHIAZOLE DIOXIDES AS CXC- AND CC- CHEMOKINE RECEPTOR LIGANDS
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Disclosed are novel compounds of the formula (IA): and the pharmaceutically acceptable salts and solvates thereof. D and E are different groups wherein one is N and the other is CR50. Examples of groups comprising Substituent A include heteroaryl, aryl, heterocycloalkyl, cycloalkyl, aryl, alkynyl, alkenyl, aminoalkyl, alkyl or amino. Examples of groups comprising Substituent B include aryl and heteroaryl. Also disclosed is a method of treating a chemokine mediated diseases, such as, cancer, angiogenisis, angiogenic ocular diseases, pulmonary diseases, multiple sclerosis, rheumatoid arthritis, osteoarthritis, stroke and cardiac reperfusion injury, pain (e.g., acute pain, acute and chronic inflammatory pain, and neuropathic pain) using a compound of formula IA.
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Page/Page column 262-263
(2010/02/13)
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- Pyridine, pyrimidine, quinoline, quinazoline, and naphthalene urotensin-II receptor antagonists
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The present invention relates to urotensin II receptor antagonists, pharmaceutical compositions containing them and their use.
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- THIADIAZOLEDIOXIDES AND THIADIAZOLEOXIDES AS CXC- AND CC-CHEMOKINE RECEPTOR LIGANDS
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Disclosed are novel compounds of the formula (IA) and the pharmaceutically acceptable salts and solvates thereof. Examples of groups comprising Substituent A include heteroaryl, aryl, heterocycloalkyl, cycloalkyl, aryl, alkynyl, alkenyl, aminoalkyl, alkyl or amino. Examples of groups comprising Substituent B include aryl and heteroaryl. Also disclosed is a method of treating a chemokine mediated diseases, such as, cancer, angiogenisis, angiogenic ocular diseases, pulmonary diseases, multiple sclerosis, rheumatoid arthritis, osteoarthritis, stroke and cardiac reperfusion injury, acute pain, acute and chronic inflammatory pain, and neuropathic pain using a compound of formula (IA).
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- 3,4-Di-substituted cyclobutene-1,2-diones as CXC-chemokine receptor ligands
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There are disclosed compounds of the formula or a pharmaceutically acceptable salt or solvate thereof which are useful for the treatment of chemokine-mediated diseases such as acute and chronic inflammatory disorders and cancer.
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- 3,4-Di-substituted cyclobutene-1,2-diones as CXC-chemokine receptor ligands
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There are disclosed compounds of the formula or a pharmaceutically acceptable salt or solvate thereof which are useful for the treatment of chemokine-mediated diseases such as acute and chronic inflammatory disorders and cancer.
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- Effect of Amine Nature on Reaction Rate and Mechanism in Nucleophilic Substitution Reactions of 2,4-Dinitrophenyl X-Substituted Benzenesulfonates with Alicyclic Secondary Amines
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Second-order rate constants have been measured for reactions of 2,4-dinitrophenyl X-substituted benzenesulfonates with a series of alicyclic secondary amines. The reaction proceeds through S-O and C-O bond fission pathways competitively. The S-O bond fission occurs more dominantly as the amine basicity increases and the substituent X in the sulfonyl moiety becomes more strongly electron withdrawing, indicating that the regioselectivity is governed by the amine basicity as well as the electronic nature of the substituent X. The S-O bond fission proceeds through an addition intermediate with a change in the rate-determining step at pKa° = 9.1. The secondary amines are more reactive than primary amines of similar basicity for the S-O bond fission. The k1 value has been determined to be larger for reactions with secondary amines than with primary amines of similar basicity, which fully accounts for their higher reactivity. The second-order rate constants for the S-O bond fission result in linear Yukawa-Tsuno plots while those for the C-O bond fission exhibit poor correlation with the electronic nature of the substituent X. The distance effect and the nature of reaction mechanism have been suggested to be responsible for the poor correlation for the C-O bond fission pathway.
- Um, Ik-Hwan,Chun, Sun-Mee,Chae, Ok-Mi,Fujio, Mizue,Tsuno, Yuho
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p. 3166 - 3172
(2007/10/03)
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- Theophylline and 3-isobutyl-1-methylxanthine based N-7 substituted derivatives displaying inhibitory activies on PDE-5 phosphodiesterase
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Compounds of the theophylline and 3-isobutyl-1-methylxanthine (IBMX) based on N-7 substituted derivatives, X being florine, chlorine, bromine or iodine, are provided. These compounds possess pharmacologically inhibitory activities on PDE-5 Phosphodiestera
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- Synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors
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A series of N1-activated C4-carboxy azetidinones was prepared and tested as inhibitors of human tryptase. The key stereochemical and functional features required for potency, serine protease specificity and aqueous stability were determined. From these studies compound 2, BMS-262084, was identified as a potent and selective tryptase inhibitor which, when dosed intratracheally in ovalbumin-sensitized guinea pigs, reduced allergen-induced bronchoconstriction and inflammatory cell infiltration into the lung.
- Sutton, James C.,Bolton, Scott A.,Hartl, Karen S.,Huang, Ming-Hsing,Jacobs, Glenn,Meng, Wei,Ogletree, Martin L.,Pi, Zulan,Schumacher, William A.,Seiler, Steven M.,Slusarchyk, William A.,Treuner, Uwe,Zahler, Robert,Zhao, Guohua,Bisacchi, Gregory S.
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p. 3229 - 3233
(2007/10/03)
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- Beta lactam compounds and their use as inhibitors of tryptase
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Compounds of the formulas: are disclosed. These compounds inhibit tryptase as well as other enzyme systems or are selective tryptase inhibitors and are useful as antiinflammatory agents particularly in the treatment of chronic asthma.
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Page column 75
(2010/11/29)
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- Theophylline and 3-isobutyl-1-methylxanthine based N-7 substituted derivatives displaying inhibitory activities on type five phosphodiesterase
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Theophylline derivative of formula I and II, Wherein R1 is —(CH2),CH3; R2 is a member selected from the group of R4 is a member selected from the group of H, —(CH2)nCH3, X, NH2 and —NO2; R5 is a member selected from the group of H, wherein R3 is a member selected from the group of halogen, hydroxyl group (OH), saturated 1-3 straight chain carbon or group substituting one hydrogen; n is 0, 1, 2 or 3. In vivo or in vitro experiments, prove the carvernosal relaxation induced by these compounds.
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- NOVEL QUINAZOLINE DERIVATIVES
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Quinazoline derivatives represented by the general formula (1) or a pharmaceutically acceptable salt thereof in said formula R1is nitro or halogen; R2and R4are each hydrogen, C1-4alkyl, carboxyl, or C2-5alkoxycarbonyl; R3is hydrogen, amino, optionally substituted C1-4alkyl, C1-4alkanoyl, or C2-5alkoxycarbonyl; W is carbon or nitrogen; and m is 0 to 2.
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- Certain substituted 1-aryl-3-piperazin-1′-yl propanones
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Disclosed are compounds of formula I: wherein X is a carbonyl, sulfonyl, methylene, or methylene substituted with optionally substituted phenyl; Z is nitrogen or CH; Ar1and Ar2independently represent aryl groups; and Y is hydrogen; o
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- Nucleophilic reactivity towards electrophilic fluorinating agents: Reaction with N-fluorobenzenesulfonimide ((PhSO2)2NF)
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Second-order rate constants for the reaction of N-fluorobenzenesulfonimide (FBS) with nucleophilic reagents, kNu (M-1 s-1), have been measured in aqueous solution at 25°C. Analysis of the reaction products shows that soft polarizable nucleophiles (I-, SCN-, Br-) react at fluorine, whereas hard nucleophiles (oxygen and nitrogen nucleophiles) react at sulfur. The ambident behaviour of this electrophile seems to be related to the relative contribution of electrostatic and orbital interactions in reaching the transition state. The preferential reaction of soft nucleophiles at fluorine and the correlation of kNu values with the one-electron oxidation potentials of the nucleophiles in water suggest that nucleophilic reactivity at fluorine is largely determined by the ease of one-electron transfer from the nucleophile to the electrophile. Nucleophilic addition to fluorine is far more sensitive to the nature of the attacking nucleophile than the corresponding reactions at both saturated (n scale) and unsaturated carbon (N+ scale). Comparison of the rate constants for the reaction of nucleophiles at the sulfonyl group with those for reaction of the same nucleophiles with 2,4-dinitrophenyl acetate reveals a similar reactivity pattern for sulfonyl sulfur and carbonyl carbon as electrophilic centres.
- Antelo, Juan M.,Crugeiras, Juan,Leis, J. Ramon,Rios, Ana
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p. 2071 - 2076
(2007/10/03)
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- Certain substituted 1-aryl-3-piperazin-1'-yl propanones to treat Alzheimer's Disease
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Disclosed are compounds of formula I: STR1 or the pharmaceutically acceptable salts thereof wherein X is a carbonyl, sulfonyl, methylene, or methylene substituted with optionally substituted phenyl; Z is nitrogen or CH; Ar1 and Ar2 i
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- Substituted 1-aryl-3-piperazin-1'-yl propanones
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Disclosed are compounds of formula I: STR1 wherein X is a carbonyl, sulfonyl, methylene, or methylene substituted with optionally substituted phenyl; Z is nitrogen or CH; Ar1 and Ar2 independently represent aryl groups; and Y is hydr
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