Synthesis of 2-substituted-6,8-dichloro-3,4-dihydro-3-oxo-2H-1,4-benzothiazine-1,1-dioxides and -1-oxides as glycine-NMDA receptor antagonists

Authors
Varano, F Catarzi, D Colotta, V Filacchioni, G Cecchi, L Galli, A Costagli, C
Citation
F. Varano et al., Synthesis of 2-substituted-6,8-dichloro-3,4-dihydro-3-oxo-2H-1,4-benzothiazine-1,1-dioxides and -1-oxides as glycine-NMDA receptor antagonists, FARMACO, 53(12), 1998, pp. 752-757
Citations number
14
Categorie Soggetti
Pharmacology & Toxicology
Journal title
FARMACO
ISSN journal
0014827X → ACNP
Volume
53
Issue
12
Year of publication
1998
Pages
752 - 757
Database
ISI
SICI code
0014-827X(199812)53:12<752:SO2>2.0.ZU;2-P
Abstract
A number of 2-substituted-3,4-dihydro-3-oxo-6,8-dichloro-2H-1,4-benzothiazi ne-1,1-dioxides (1-2a-b) and -1-oxides (3-4a-b) bioisosters of RPR 104632 i n which the 3-carboxylic group was replaced by a carbonyl group were synthe sized. Comparative in vitro pharmacological studies on this series of RPR 1 04632 analogs were performed using receptor binding assays. None of these c ompounds showed detectable binding affinity for the glycine-NMDA receptor. (C) 1998 Elsevier Science S.A. All rights reserved.