Article
Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitor Agents: Optimization of Diarylanilines with High Potency against Wild-Type and Rilpivirine-Resistant E138K Mutant Virus.
Journal of medicinal chemistry - 28 Apr 2016
Liu Na, Wei Lei, Huang Li, Yu Fei, Zheng Weifan, Qin Bingjie, Zhu Dong-Qin, Morris-Natschke Susan L, Jiang Shibo, Chen Chin-Ho, Lee Kuo-Hsiung, Xie Lan
Abstract excerpt
Three series (6, 13, and 14) of new diarylaniline (DAAN) analogues were designed, synthesized, and evaluated for anti-HIV potency, especially against the E138K viral strain with a major mutation conferring resistance to the new-generation non-nucleoside reverse transcriptase inhibitor drug rilpivirine (1b). Promising new compounds were then assessed for physicochemical and associated pharmaceutical properties,...
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