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Discovery of nitropyridine derivatives as potent HIV-1 non-nucleoside reverse transcriptase inhibitors via a structure-based core refining approach

…, Z Li, H Liu, E De Clercq, C Pannecouque, X Liu

文献索引:Wang, Jun; Zhan, Peng; Li, Zhenyu; Liu, Huiqing; De Clercq, Erik; Pannecouque, Christophe; Liu, Xinyong European Journal of Medicinal Chemistry, 2014 , vol. 76, p. 531 - 538

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被引用次数: 10

摘要

Abstract As a continuation of our efforts to discover and develop back-up analogs of DAPYs, novel substituted nitropyridine derivatives were designed via a structure-based core refining approach, synthesized and evaluated for their in vitro HIV-1 activity in MT-4 cells. Preliminary biological evaluation indicated that most of the compounds exhibited marked inhibitory activity against wild-type HIV-1 III B. Most notably, the compound 7b was ...