Optimization of diarylamines as non-nucleoside inhibitors of HIV-1 reverse transcriptase

Optimization of diarylamines as non-nucleoside inhibitors of HIV-1 reverse transcriptase
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DOI:
10.1016/j.bmcl.2005.10.037
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发表时间:
2006-02-01
影响因子:
2.7
通讯作者:
Jorgensen, WL
Jorgensen, WL
中科院分区:
医学4区
文献类型:
--
作者:
Ruiz-Caro, J;Basavapathruni, A;Jorgensen, WL

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在计算分析之后,通过合成和测定抗病毒活性来寻求HIV-1逆转录酶的潜在非核苷抑制剂。一般类Het-NH-Ph-U已被考虑,其中Het是芳香杂环和U是不饱和的,疏水基团。Het = 2-噻唑基和2-嘧啶基的化合物的结果是本报告的重点。(c)2005爱思唯尔有限公司保留所有权利。
Following computational analyses, potential non-nucleoside inhibitors of HIV-1 reverse transcriptase have been pursued through synthesis and assaying for anti-viral activity. The general class Het-NH-Ph-U has been considered, where Het is an aromatic heterocycle and U is an unsaturated, hydrophobic group. Results for compounds with Het = 2-thiazoyl and 2-pyrimidinyl are the focus of this report. (c) 2005 Elsevier Ltd. All rights reserved.