Potent, selective 3-pyridylethanolamine beta3 adrenergic receptor agonists possessing a thiazole benzenesulfonamide pharmacophore |
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| Authors: | Mathvink R J Tolman J S Chitty D Candelore M R Cascieri M A Colwell L F Deng L Feeney W P Forrest M J Hom G J MacIntyre D E Tota L Wyvratt M J Fisher M H Weber A E |
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| Affiliation: | Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA. robert_mathvink@merck.com |
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| Abstract: | ![]()
A series of thiazole benzenesulfonamide-substituted 3-pyridylethanolamines was prepared and evaluated for their human beta3 adrenergic receptor agonist activity. Incorporation of aryl and heteroaryl substitution in the 4-position of the thiazole ring resulted in a number of highly potent and selective beta3 agonists. Results of preliminary in vivo evaluation of several of these compounds is described. |
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