Çakir Gizem, Küçükgüzel İlkay, Guhamazumder Rupa, Tatar Esra, Manvar Dinesh, Basu Amartya, Patel Bhargav A, Zia Javairia, Talele Tanaji T, Kaushik-Basu Neerja
Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Marmara University, Haydarpaşa, İstanbul, Turkey.
Arch Pharm (Weinheim). 2015 Jan;348(1):10-22. doi: 10.1002/ardp.201400247. Epub 2014 Dec 2.
In continuation of our efforts to develop new derivatives as hepatitis C virus (HCV) NS5B inhibitors, we synthesized novel 5-arylidene-4-thiazolidinones. The novel compounds 29-42, together with their synthetic precursors 22-28, were tested for HCV NS5B inhibitory activity; 12 of these compounds displayed IC50 values between 25.3 and 54.1 µM. Compound 33, an arylidene derivative, was found to be the most active compound in this series with an IC50 value of 25.3 µM. Molecular docking studies were performed on the thumb pocket-II of NS5B to postulate the binding mode for these compounds.
为持续努力开发新型衍生物作为丙型肝炎病毒（HCV）NS5B抑制剂，我们合成了新型5-亚芳基-4-噻唑烷酮。对新型化合物29 - 42及其合成前体22 - 28进行了HCV NS5B抑制活性测试；其中12种化合物的IC50值在25.3至54.1μM之间。芳亚基衍生物化合物33被发现是该系列中活性最高的化合物，IC50值为25.3μM。对NS5B的拇指口袋-II进行了分子对接研究，以推测这些化合物的结合模式。
