Novel 2,2-dioxide-4,4-disubstituted-1,3-H-2,1,3-benzothiadiazines as non-nucleoside reverse transcriptase inhibitors

被引：26

作者：

Corbett, JW ^{[1
]}

Gearhart, LA ^{[1
]}

Ko, SS ^{[1
]}

Rodgers, JD ^{[1
]}

Cordova, BC ^{[1
]}

Klabe, RM ^{[1
]}

Erickson-Viitanen, SK ^{[1
]}

机构：

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 02期

关键词：

D O I：

10.1016/S0960-894X(99)00672-1

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Benzothiadiazine non-nucleoside reverse transcriptase inhibitors (NNRTIs) of HIV have been synthesized via a novel process to afford active inhibitors, with the most potent compound exhibiting an IC90 = 180 nM in a whole cell assay. The 2,2-dioxide- 1H-2,1,3 -benzothiadiazine ring system was constructed in one step from 2-amino-5-chlorobenzonitrile. (C) 2000 DuPont Pharmaceuticals Company. Published by Elsevier Science Ltd. All rights reserved.

引用

页码：193 / 195

页数：3

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