Potent, selective 3-pyridylethanolamine beta3 adrenergic receptor agonists possessing a thiazole benzenesulfonamide pharmacophore

R J Mathvink; J S Tolman; D Chitty; M R Candelore; M A Cascieri; L F Colwell Jr; L Deng; W P Feeney; M J Forrest; G J Hom; D E MacIntyre; L Tota; M J Wyvratt; M H Fisher; A E Weber

doi:10.1016/s0960-894x(00)00390-5

Potent, selective 3-pyridylethanolamine beta3 adrenergic receptor agonists possessing a thiazole benzenesulfonamide pharmacophore

Bioorg Med Chem Lett. 2000 Sep 4;10(17):1971-3. doi: 10.1016/s0960-894x(00)00390-5.

Authors

R J Mathvink¹, J S Tolman, D Chitty, M R Candelore, M A Cascieri, L F Colwell Jr, L Deng, W P Feeney, M J Forrest, G J Hom, D E MacIntyre, L Tota, M J Wyvratt, M H Fisher, A E Weber

Affiliation

¹ Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA. [email protected]

PMID: 10987429
DOI: 10.1016/s0960-894x(00)00390-5

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.

MeSH terms

Adrenergic beta-3 Receptor Agonists*
Adrenergic beta-Agonists / chemical synthesis*
Adrenergic beta-Agonists / pharmacology
Animals
Benzenesulfonamides
CHO Cells
Cricetinae
Ethanolamines / chemical synthesis*
Humans
Structure-Activity Relationship
Sulfonamides / chemical synthesis*
Thiazoles / chemical synthesis*

Substances

Adrenergic beta-3 Receptor Agonists
Adrenergic beta-Agonists
Ethanolamines
Sulfonamides
Thiazoles