Antiviral 2,5-disubstituted imidazo[4,5-c]pyridines: Further optimization of anti-hepatitis C virus activity
作者:Gerhard Puerstinger、Jan Paeshuyse、Susanne Heinrich、Joachim Mohr、Nicole Schraffl、Erik De Clercq、Johan Neyts
DOI:10.1016/j.bmcl.2007.07.015
日期:2007.9
zo[4,5-c]pyridines represent a novel class of compounds with activity against pestiviruses and the hepatitis C virus (HCV). Several series of analogues with modifications of the substituents in positions 2 and 5 were prepared. These efforts resulted in the discovery of several compounds with potent antiviral activity of which 2-(2,3-difluorophenyl)-5-[4-(trifluoromethyl)benzyl]-5H-imidazo[4,5-c]pyridine
取代的5-苄基-2-苯基-5H-咪唑并[4,5-c]吡啶代表了一类新的对瘟病毒和丙型肝炎病毒(HCV)具有活性的化合物。制备了几个在位置2和5上具有取代基修饰的类似物系列。这些努力导致发现了几种具有有效抗病毒活性的化合物,其中2-(2,3-二氟苯基)-5- [4-(三氟甲基)苄基] -5H-咪唑并[4,5-c]吡啶(46)对HCV最有效(EC(50)为0.10 microM,选择性指数为1080)。