4-Hydroxy-5-pyrrolinone-3-carboxamide HIV-1 integrase inhibitors

被引：36

作者：

Pace, Paola ^{[1
]}

Spieser, Stephane A. H. ^{[1
]}

Summa, Vincenzo ^{[1
]}

机构：

[1] IRBM, MRL Rome, Dept Med Chem, I-00040 Pomezia, Italy

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 14期

关键词：

AIDS; HIV-1; integrase; Diketoacids; pyrimidines; pyrrolinones;

D O I：

10.1016/j.bmcl.2008.06.056

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The viral enzyme integrase is essential for the replication of HIV-1 and, after the discovery of Isentress (TM), represents a validated target for anti-retroviral therapy. Incorporation of the dihydroxycarbonyl pharmacophore into a pyrrolinone scaffold led to the discovery of 5-pyrrolinone-3-carboxamides as a structurally diverse class of HIV-1 integrase inhibitors. (C) 2008 Elsevier Ltd. All rights reserved.

引用

页码：3865 / 3869

页数：5

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