Article
Discovery of imidazo[2,1-b]thiazole HCV NS4B inhibitors exhibiting synergistic effect with other direct-acting antiviral agents.
Journal of medicinal chemistry - 26 Mar 2015
Wang Ning-Yu, Xu Ying, Zuo Wei-Qiong, Xiao Kun-Jie, Liu Li, Zeng Xiu-Xiu, You Xin-Yu, Zhang Li-Dan, Gao Chao, Liu Zhi-Hao, Ye Ting-Hong, Xia Yong, Xiong Ying, Song Xue-Jiao, Lei Qian, Peng Cui-Ting, Tang Hong, Yang Sheng-Yong, Wei Yu-Quan, Yu Luo-Ting
Abstract excerpt
The design, synthesis, and SAR studies of novel inhibitors of HCV NS4B based on the imidazo[2,1-b]thiazole scaffold were described. Optimization of potency with respect to genotype 1b resulted in the discovery of two potent leads 26f (EC50 = 16 nM) and 28g (EC50 = 31 nM). The resistance profile studies revealed that 26f and 28g targeted HCV NS4B, more precisely the second amphipathic α helix of NS4B (4BAH2)....
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