Arylalkylidene rhodanine with bulky and hydrophobic functional group as selective HCV NS3 protease inhibitor

WT Sing, CL Lee, SL Yeo, SP Lim, MM Sim

Index: Sing, Wan Theng; Lee, Cheng Leng; Yeo, Su Ling; Lim, Siew Pheng; Sim, Mui Mui Bioorganic and Medicinal Chemistry Letters, 2001 , vol. 11, # 2 p. 91 - 94

Full Text: HTML

Citation Number: 123

Abstract

Arylalkylidene rhodanines 2 (a–d) inhibit HCV NS3 protease at moderate concentrations. They are better inhibitors of other serine proteases such as chymotrypsin and plasmin. However, the selectivity of arylmethylidene rhodanines (8a, 9a) with bulkier and more hydrophobic functional groups increases by 13-and 25-fold towards HCV NS3 protease respectively.