Synthesis and evaluation of benzoxazinones as HIV-1 reverse transcriptase inhibitors.: Analogs of Efavirenz (SUSTIVA™)

被引：92

作者：

Patel, M ^{[1
]}

McHugh, RJ ^{[1
]}

Cordova, BC ^{[1
]}

Klabe, RM ^{[1
]}

Erickson-Viitanen, S ^{[1
]}

Trainor, GL ^{[1
]}

Ko, SS ^{[1
]}

机构：

[1] DuPont Pharmaceut Co, Expt Stn, Wilmington, DE 19880 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1999年 / 9卷 / 22期

关键词：

D O I：

10.1016/S0960-894X(99)00565-X

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Two series of benzoxazinones differing in the aromatic substitution pattern were prepared and evaluated as HIV-1 reverse transcriptase inhibitors. The 5-fluoro (5a-d) and 6-nitro (5e-h) substituted compounds displayed activity comparable or better than Efavirenz, the lead structure of the series. (C) 1999 DuPont Pharmaceuticals Company. Published by Elsevier Science Ltd. All rights reserved.

引用

页码：3221 / 3224

页数：4

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