alpha(2) adrenoceptor agonists as potential analgesic agents. 1. (Imidazolylmethyl)oxazoles and -thiazoles

Citation
Re. Boyd et al., alpha(2) adrenoceptor agonists as potential analgesic agents. 1. (Imidazolylmethyl)oxazoles and -thiazoles, J MED CHEM, 42(25), 1999, pp. 5064-5071
Citations number
39
Categorie Soggetti
Chemistry & Analysis
Journal title
JOURNAL OF MEDICINAL CHEMISTRY
ISSN journal
00222623 → ACNP
Volume
42
Issue
25
Year of publication
1999
Pages
5064 - 5071
Database
ISI
SICI code
0022-2623(199912)42:25<5064:AAAAPA>2.0.ZU;2-J
Abstract
A series of (imidazolylmethyl)oxazoles and -thiazoles were prepared and eva luated as alpha(2) adrenoceptor agonists. These compounds were also tested in in vivo paradigms that are predictive of analgesic activity. Variations in both the imidazole and thiazole portions of the molecule were investigat ed. Some of the more potent compounds such as 22, 26, 45, and 53 displayed at receptor binding in the 10-20 nM range and also had significant, antinoc iceptive activity in the mouse abdominal irritant test (MAIT).