α2 Adrenoceptor Agonists as Potential Analgesic Agents. 1. (Imidazolylmethyl)oxazoles and -thiazoles
Journal of Medicinal Chemistry1999Vol. 42(25), pp. 5064–5071
Citations Over Time
Robert E. Boyd, Jeffery B. Press, C. Royce Rasmussen, Robert B. Raffa, Ellen E. Codd, Charlene D. Connelly, Debra J. Bennett, Alex L. Kirifides, Joseph F. Gardocki, Brian Reynolds, John T. Hortenstein, Allen B. Reitz
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).
Related Papers
- → 3-Arylsulphonyl-5-arylamino-1,3,4-thiadiazol-2(3H)ones as anti-inflammatory and analgesic agents(2001)70 cited
- → EVALUATION OF ANTI-INFLAMMATORY AND ANALGESIC ACTIVITY OF NOVEL PYRAZOLE DERIVATIVES(2014)7 cited
- → Synthesis of long chain lipid amides and their analgesic properties(2018)2 cited
- → Don't ignore non-pharmacological aspects of analgesia while pursuing analgesic success(2013)
- → F148 EXPERIENCE WITH ANALGESIC AGENTS SHAPES THE EFFICACY OF UNRELATED SUBSEQUENT ANALGESIC TREATMENT(2011)