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
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).