Substituted 2-pyrrolinone inhibitors of HIV-1 integrase

被引：26

作者：

Dayam, Raveendra ^{[1
]}

Al-Mawsawi, Laith Q. ^{[1
]}

Neamati, Nouri ^{[1
]}

机构：

[1] Univ So Calif, Sch Pharm, Dept Pharmaceut Sci & Pharmacol, Los Angeles, CA 90089 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 22期

关键词：

HIV-1; integrase; beta-diketoacids; pharmacophore; substituted pyrrolin-2-ones; substructure; structure-activity relationship analysis;

D O I：

10.1016/j.bmcl.2007.09.061

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The beta-diketoacid class of HIV-1 integrase (IN) inhibitors represent the first potent class of compounds specific for the strand transfer catalytic activity of the viral enzyme. Previously, utilizing a beta-diketoacid pharmacophore as a search query, we identified a substituted 2-pyrrolinone with modest IN inhibitory activity from a database of small-molecules [Dayam, R.; Sanchez, T.; Neamati, N. J. Med. Chem. 2005, 48, 8009]. In efforts to optimize this class of IN inhibitors, we carried out a structure-activity relationship analysis around the 2-pyrrolinone core. Here, we present a new class of 2-pyrrolinone IN inhibitors. (C) 2007 Elsevier Ltd. All rights reserved.

引用

页码：6155 / 6159

页数：5

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