Synthesis and evaluation of analogs of Efavirenz (SUSTIVA™) as HIV-1 reverse transcriptase inhibitors

被引：84

作者：

Patel, M ^{[1
]}

Ko, SS ^{[1
]}

McHugh, RJ ^{[1
]}

Markwalder, JA ^{[1
]}

Srivastava, AS ^{[1
]}

Cordova, BC ^{[1
]}

Klabe, RM ^{[1
]}

Erickson-Viitanen, S ^{[1
]}

Trainor, GL ^{[1
]}

Seitz, SP ^{[1
]}

机构：

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1999年 / 9卷 / 19期

关键词：

D O I：

10.1016/S0960-894X(99)00486-2

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Efavirenz (SUSTIVA(TM)) is a potent non-nucleoside reverse transcriptase inhibitor. Due to the observation of breakthrough mutations of the reverse transcriptase enzyme during Efavirenz therapy, we sought to develop an optimized second generation series. To that end, SAR of the substituents on the aromatic ring was undertaken and the results are summarized here. The 5,6-difluoro (4f) and the 6-methoxy (4m) substituted benzoxazinones were determined to be equipotent, and as a result such substitution patterns will be incorporated in second generation scaffolds. (C) 1999 DuPont Pharmaceuticals. Published by Elsevier Science Ltd. All rights reserved.

引用

页码：2805 / 2810

页数：6

共 7 条

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