Structural modification of diarylpyrimidine derivatives as HIV-1 reverse transcriptase inhibitors

被引：0
作者：
Shuang-Xi Gu
Yuan-Yuan Zhu
Fen-Er Chen
Erik De Clercq
Jan Balzarini
Christophe Pannecouque
机构：
[1] Wuhan Institute of Technology,Key Laboratory for Green Chemical Process of Ministry of Education and School of Chemical Engineering and Pharmacy
[2] Wuhan Institute of Technology,School of Chemistry and Environmental Engineering
[3] Fudan University,Department of Chemistry
[4] Katholieke Universiteit Leuven,Rega Institute for Medical Research
来源：
Medicinal Chemistry Research | 2015年 / 24卷
关键词：
HIV-1; Reverse transcriptase inhibitors; Diarylpyrimidines;
D O I：
暂无
中图分类号：
学科分类号：
摘要：
As a continuing and exploratory work on diarylpyrimidines (DAPYs) as human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (RT) inhibitors, bulky and electron-rich naphthyl was introduced into the structure of DAPYs to replace the phenyl left wing of DAPYs, which is aimed to improve the π–π stacking interactions between inhibitors and some aromatic amino acid residues within the binding pocket of RT. The title compound 1a, with a 1-naphthyl left wing, displayed good inhibitory activity against wild-type HIV-1 (EC50 = 0.071 μM), along with moderate inhibitory activity against HIV-2 (EC50 = 6.5 μM).
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页码：220 / 225
页数：5
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