- Discovery and structure-activity relationships study of novel thieno[2,3-b]pyridine analogues as hepatitis C virus inhibitors
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Current treatment for hepatitis C is barely satisfactory, there is an urgent need to develop novel agents for combating hepatitis C virus infection. This study discovered a new class of thieno[2,3-b]pyridine derivatives as HCV inhibitors. First, a hit compound characterized by a thienopyridine core was identified in a cell-based screening of our privileged small molecule library. And then, structure activity relationship study of the hit compound led to the discovery of several potent compounds without obvious cytotoxicity in vitro (12c, EC50 = 3.3 μM, SI >30.3, 12b, EC50 = 3.5 μM, SI >28.6, 10l, EC50 = 3.9 μM, SI >25.6, 12o, EC 50 = 4.5 μM, SI >22.2, respectively). Although the mechanism of them had not been clearly elucidated, our preliminary optimization of this class of compounds had provided us a start point to develop new anti-HCV agents.
- Wang, Ning-Yu,Zuo, Wei-Qiong,Xu, Ying,Gao, Chao,Zeng, Xiu-Xiu,Zhang, Li-Dan,You, Xin-Yu,Peng, Cui-Ting,Shen, Yang,Yang, Sheng-Yong,Wei, Yu-Quan,Yu, Luo-Ting
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p. 1581 - 1588
(2014/03/21)
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- Enaminones as building blocks in heterocyclic syntheses: Reinvestigating the product structures of enaminones with malononitrile. A novel route to 6-substituted-3-oxo-2,3-dihydropyridazine-4-carboxylic acids
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The reported structures of reaction products of enaminones with malononitrile in ethanolic piperidine are revised. A novel route to 2,3-dihydropyridazine-4-carboxylic acids 4a-c via reactions of 2-cyano-5-(dimethylamino)-5-arylpenta-2,4-dienamides 8a-c wi
- Alnajjar, Abdul-Aziz,Abdelkhalik, Mervat Mohammed,Al-Enezi, Amal,Elnagdi, Mohamed Hilmy
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experimental part
p. 68 - 77
(2009/08/15)
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- About the reaction of β-dimethylamino-α,β-enones with active methylene nitriles
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(Chemical Equation Presented) The reaction of 3-dimethylamino-1- arylpropenone derivatives with active methylene nitriles was reinvestigated and a plausible mechanism to account for the results is suggested. X-ray crystallographic study supported the sugg
- Abdelrazek, Fathy M.,Elsayed, Akram N.
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experimental part
p. 949 - 953
(2009/12/05)
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- 2-Aminopyridine compounds and use thereof as drugs
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The present invention provides 2-aminopyridine compound having an excellent adenosine receptor (A1, A2a, A2b receptors) antagonism, which is represented by the following formula: (wherein, R1 represents cyano gr
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- 2-AMINOPYRIDINE COMPOUNDS AND USE THEREOF AS DRUGS
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The present invention provides 2-aminopyridine compound having an excellent adenosine receptor (A1, A2a, A2b receptors) antagonism, which is represented by the following formula: (wherein, R1 represents cyano gr
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- Substituted N-(1,2-dihydro-2-oxonicotinyl)-cephalexins and -cephaloglycins
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Novel organic amide compounds which are substituted N-(1,2-dihydro-2-oxonicotinyl)-ampicillins, -cephalexins and -cephaloglycins having broad spectrum antibacterial utility are provided by (a) reacting the free amino acid ampicillin, cephalexin or cephaloglycin or the acid salt or silylated derivative thereof with a reactive derivative of the corresponding 1,2-dihydro-2-oxonicotinic acid or (b) reacting the free amino acid 6-aminopenicillanic acid, 7-aminocephalosporanic acid or 7-amino-3-methylceph-3-em-4-carboxylic acid or the acid salt or silylated derivative thereof with a reactive derivative of the corresponding N-(1,2-dihydro-2-oxonicotinyl)-2-phenylglycine.
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