54364-12-4Relevant academic research and scientific papers
Discovery and structure-activity relationships study of novel thieno[2,3-b]pyridine analogues as hepatitis C virus inhibitors
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
, p. 1581 - 1588 (2014/03/21)
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.
SUBSTITUTED PYRIDO[3',2':4,5]THIENO[3,2-D]PYRIMIDINE-2,4(1 H,3H)-DIONES AND -4(3H)-ONES, SUBSTITUTED THIENO[2,3-D:4,5-D']DIPYRIMIDINE-2,4(1 H,3H)-DIONES AND -4(3H)-ONES, SUBSTITUTED PYRIDO[3',2':4,5]FURO[3,2-D]PYRIMIDINE-2,4(1 H,3H)-DIONES AND -4(3H)-ONES, AND SUBSTITUTED FURO[2,3-D:4,5-D']DIPYRIMIDINE-2,4(1 H,3H)-DIONES AN
-
Page/Page column 68, (2010/02/15)
The invention relates to novel pyrido[3',2':4,5]thieno[3,2-d]pyrimidine-2,4(1 H,3H)-diones and -4(3H)-one (X=C-H, Y=S), thieno[2,3-d:4,5-d']dipyrimidine-2,4(1 H,3H)-diones and -4(3H)-one (X=N, Y=S), in addition to pyrido[3',2':4,5]furo[3,2-d]pyrimidine-2,4(1 H,3H)-diones and -4(3H)-one (X=C-H, Y=0) and furo[2,3-d:4,5-d']dipyrimidine-2,4(1 H,3H)-diones and -4(3H)-one (X=N, Y=O) of general formulae 1a and 1b. The invention also relates to a method for the production thereof, pharmaceutical preparations containing said compounds and/or tautomers thereof and physiologically compatible salts which can be produced therefrom and/or solvates thereof, in addition to the pharmaceutical use of said compounds, tautomers thereof, salts or solvates, as inhibitors of TNFa-release.
