Novel potent inhibitors of hepatitis C virus (HCV) NS3 protease with cyclic sulfonyl P3 cappings

KX Chen, B Vibulbhan, W Yang, LG Nair, X Tong…

文献索引：Chen, Kevin X.; Vibulbhan, Bancha; Yang, Weiying; Nair, Latha G.; Tong, Xiao; Cheng, Kuo-Chi; Njoroge, F. George Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 4 p. 1105 - 1109

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被引用次数: 14

摘要

Extensive SAR studies of the P3 capping group led to the discovery of a series of potent inhibitors with sultam and cyclic sulfonyl urea moieties as the P3 capping. The bicyclic thiophene-sultam or phenyl-sultam cappings were selected for further SAR development. Modification at the P3 side chain determined that the tert-butyl group was the best choice at that position. Optimization of P1 residue significantly improved potency and selectivity. ...