Synthesis, Biological Evaluation and Molecular Modeling Studies of N??aryl??2??arylthioacetamides as Non??nucleoside HIV??1 Reverse Transcriptase Inhibitors

…, Q Yu, Y Hong, S Xiuqing, Z Rugang

文献索引：Xiaohe, Zhu; Yu, Qin; Hong, Yan; Xiuqing, Song; Rugang, Zhong Chemical Biology and Drug Design, 2010 , vol. 76, # 4 p. 330 - 339

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被引用次数: 5

摘要

A series of N-aryl-2-arylthioacetamide derivatives (2–4) designed as non-nucleoside reverse transcriptase inhibitors was synthesized and evaluated for their inhibitory activity against HIV-1 (IIIB) replication in MT-4 cell cultures. The compounds 2–4 were performed by the reaction of thiols and 2-chloro-N-substituted-acetamides and active in the lower micromolar concentration (1.25–20.83 lM). The studies of structure–activity relationship ...