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

Authors
Corbett, JW Gearhart, LA Ko, SS Rodgers, JD Cordova, BC Klabe, RM Erickson-Viitanen, SK
Citation
Jw. Corbett et al., Novel 2,2-dioxide-4,4-disubstituted-1,3-H-2,1,3-benzothiadiazines as non-nucleoside reverse transcriptase inhibitors, BIOORG MED, 10(2), 2000, pp. 193-195
Citations number
8
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
2
Year of publication
2000
Pages
193 - 195
Database
ISI
SICI code
0960-894X(20000117)10:2<193:N2AN>2.0.ZU;2-5
Abstract
Benzothiadiazine non-nucleoside reverse transcriptase inhibitors (NNRTIs) o f 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 constru cted in one step from 2-amino-5-chlorobenzonitrile. (C) 2000 DuPont Pharmac euticals Company. Published by Elsevier Science Ltd. All rights reserved.