Lead Optimization of Diarylpyrimidines as Non-nucleoside Inhibitors of HIV-1 Reverse Transcriptase

被引:31
作者
Zeng, Zhao-Sen [1 ]
Liang, Yong-Hong [1 ]
Feng, Xiao-Qing [1 ]
Chen, Fen-Er [1 ,2 ]
Pannecouque, Christophe [3 ]
Balzarini, Jan [3 ]
De Clercq, Erik [3 ]
机构
[1] Fudan Univ, Dept Chem, Shanghai 200433, Peoples R China
[2] Fudan Univ, Inst Biomed Sci, Shanghai 200433, Peoples R China
[3] Katholieke Univ Leuven, Rega Inst Med Res, B-3000 Louvain, Belgium
基金
中国国家自然科学基金;
关键词
HIV-1; inhibitors; NNRTI; reverse transcriptase; structure-activity relationships; POSITIONAL ADAPTABILITY; ANTIVIRAL ACTIVITY; WILD-TYPE; DESIGN; ANALOGS; DRUG; ETRAVIRINE; POTENT; SAR;
D O I
10.1002/cmdc.201000045
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Antiviral agents: A series of CN-CH2-DAPY analogues were identified as novel non-nucleoside reverse transcriptase inhibitors (NNRTIs) against HIV-1. Most of the newly synthesized compounds exhibited strong activity against wild-type HIV-1. © 2010 Wiley-VCH Verlag GmbH & Co. KGaA.
引用
收藏
页码:837 / 840
页数:4
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