Amide-containing diketoacids as HIV-1 integrase inhibitors: Synthesis, structure-activity relationship analysis, and biological activity

被引：16
|
作者：
Li, Hongcai [1 ]
Wang, Chao [1 ,2 ]
Sanchez, Tino
Tan, Yanmei [1 ]
Jiang, Chunying [1 ]
Neamati, Nouri [2 ]
Zhao, Guisen [1 ]
机构：
[1] Shandong Univ, Sch Pharmaceut Sci, Jinan 250012, Shandong, Peoples R China
[2] Univ So Calif, Sch Pharm, Dept Pharmaceut Sci, Los Angeles, CA 90089 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY | 2009年 / 17卷 / 07期
基金：
中国国家自然科学基金;
关键词：
HIV; Integrase inhibitors; Diketoacids; Structure-activity relationship; SERIES;
D O I：
10.1016/j.bmc.2009.01.077
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
HIV-1 integrase, which catalyzes the integration of the viral genome into the cellular chromosome, is an essential enzyme for retroviral replication, and represents an attractive and validated target in the development of therapeutics against AIDS. In this paper, 17 amide-containing novel diketoacids were designed and synthesized, and their ability to inhibit HIV-1 integrase was tested. The structure-activity relationships were also analyzed. (C) 2009 Elsevier Ltd. All rights reserved.
引用
收藏
页码：2913 / 2919
页数：7
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