Article
Optimization of the antiviral potency and lipophilicity of halogenated 2,6-diarylpyridinamines as a novel class of HIV-1 NNRTIS.
ChemMedChem - 1 Jul 2014
Wu Zhi-Yuan, Liu Na, Qin Bingjie, Huang Li, Yu Fei, Qian Keduo, Morris-Natschke Susan L, Jiang Shibo, Chen Chin Ho, Lee Kuo-Hsiung, Xie Lan
Abstract excerpt
Nineteen new halogenated diarylpyridinamine (DAPA) analogues modified at the phenoxy C-ring were synthesized and evaluated for anti-HIV activity and certain drug-like properties. Ten compounds showed high anti-HIV activity (EC50 <10 nM). In particular, (E)-6-(2''-bromo-4''-cyanovinyl-6''-methoxy)phenoxy-N(2) -(4'-cyanophenyl)pyridin-2,3-diamine (8 c) displayed low-nanomolar antiviral potency (3-7 nM) against...
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