新型抗HIV-1药物N-芳基吡咯烷酮的合成与评价。第1部分。

Synthesis and evaluation of N-aryl pyrrolidinones as novel anti-HIV-1 agents. Part 1.

作者信息

Wu Baogen, Kuhen Kelli, Ngoc Nguyen Truc, Ellis David, Anaclerio Beth, He Xiaohui, Yang Kunyong, Karanewsky Donald, Yin Hong, Wolff Karen, Bieza Kimberly, Caldwell Jeremy, He Yun

机构信息

Genomics Institute of the Novartis Research Foundation, GNF, 10675 John Jay Hopkins Dr. San Diego, CA 92121, USA.

出版信息

Bioorg Med Chem Lett. 2006 Jul 1;16(13):3430-3. doi: 10.1016/j.bmcl.2006.04.012. Epub 2006 Apr 24.

DOI:10.1016/j.bmcl.2006.04.012

PMID:16632349

Abstract

The synthesis and preliminary structure-activity relationship of a series of pyrrolidinones are described. These pyrrolidinones have been characterized as novel non-nucleoside reverse transcriptase inhibitors (NNRTIs) which are highly potent against wild-type and drug-resistant human immunodeficiency viruses (HIV-1).

摘要

描述了一系列吡咯烷酮的合成及其初步构效关系。这些吡咯烷酮已被表征为新型非核苷类逆转录酶抑制剂（NNRTIs），对野生型和耐药性人类免疫缺陷病毒（HIV-1）具有高效活性。