SYNTHESIS AND INHIBITORY EFFECTS ON PLATELET-AGGREGATION OF 3-(2-THIENYL)- AND 3-(1-IMIDAZOLYL)-1,2-BENZISOXAOLE DERIVATIVES

Authors
NUHRICH A VARACHELEMBEGE M RENARD P DEVAUX G
Citation
A. Nuhrich et al., SYNTHESIS AND INHIBITORY EFFECTS ON PLATELET-AGGREGATION OF 3-(2-THIENYL)- AND 3-(1-IMIDAZOLYL)-1,2-BENZISOXAOLE DERIVATIVES, European journal of medicinal chemistry, 29(1), 1994, pp. 75-83
Citations number
21
Categorie Soggetti
Chemistry Medicinal
Journal title
European journal of medicinal chemistry → ACNP
ISSN journal
02235234
Volume
29
Issue
1
Year of publication
1994
Pages
75 - 83
Database
ISI
SICI code
0223-5234(1994)29:1<75:SAIEOP>2.0.ZU;2-4
Abstract
A series of 3-(2-thienyl)- and 3-(1-imidazolyl)-1,2-benzisoxazoles as well as some isomeric benzoxazoles were synthesized and tested in vitr o for their inhibitory effect on arachidonic acid-induced human platel et aggregation. The most active compound (7-methoxy-3-(2-thienyl)-1,2- benzisoxazole 5c) was nearly 20-30-fold more potent than acetylsalicyl ic acid in inhibiting platelet aggregation. Structure-activity relatio nships within the series are briefly discussed.