ID: ALA1132495
Journal: J Med Chem
Title: Alpha(2) adrenoceptor agonists as potential analgesic agents. 1. (Imidazolylmethyl)oxazoles and -thiazoles.
Authors: Boyd RE, Press JB, Rasmussen CR, Raffa RB, Codd EE, Connelly CD, Bennett DJ, Kirifides AL, Gardocki JF, Reynolds B, Hortenstein JT, Reitz AB.
Abstract: A series of (imidazolylmethyl)oxazoles and -thiazoles were prepared and evaluated 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 investigated. Some of the more potent compounds such as 22, 26, 45, and 53 displayed alpha(2) receptor binding in the 10-20 nM range and also had significant antinociceptive activity in the mouse abdominal irritant test (MAIT).
CiteXplore: 10602691
DOI: 10.1021/jm990005a
Patent ID: ┄