Design and synthesis of novel pyrimidone analogues as HIV-1 integrase inhibitors

被引：10
|
作者：
Yu, Shenghui [1 ]
Sanchez, Tino Wilson [2 ]
Liu, Yang [1 ]
Yin, Yanzhen [1 ]
Neamati, Nouri [2 ]
Zhao, Guisen [1 ]
机构：
[1] Shandong Univ, Dept Med Chem, Key Lab Chem Biol, Minist Educ,Sch Pharmaceut Sci, Jinan 250012, Shandong, Peoples R China
[2] Univ So Calif, Sch Pharm, Dept Pharmacol & Pharmaceut Sci, Los Angeles, CA 90089 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2013年 / 23卷 / 22期
基金：
中国国家自然科学基金;
关键词：
HIV-1; Integrase inhibitors; Pyrimidone analogues; POTENT; RALTEGRAVIR; DISCOVERY; UPDATE; SERIES;
D O I：
10.1016/j.bmcl.2013.09.018
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of novel pyrimidone analogues have been designed and synthesized as HIV-1 integrase (IN) inhibitors. This study demonstrated that introducing a substituent in the N1-position of the pyrimidone scaffold does not significantly influence IN inhibitory activity. Molecular docking studies showed these compounds could occupy the IN active site and form pi-pi interactions with viral DNA nucleotides DC16 and DA17 to displace reactive viral DNA 3'OH and block intasome activity. (c) 2013 Elsevier Ltd. All rights reserved.
引用
收藏
页码：6134 / 6137
页数：4
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