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Potent, elective human beta3 adrenergic receptor agonists containing a substituted indoline-5-sulfonamide pharmacophore
Journal article   Peer reviewed

Potent, elective human beta3 adrenergic receptor agonists containing a substituted indoline-5-sulfonamide pharmacophore

R J Mathvink, A M Barritta, M R Candelore, M A Cascieri, L Deng, L Tota, C D Strader, M J Wyvratt, M H Fisher and A E Weber
Bioorganic & medicinal chemistry letters, Vol.9(13), pp.1869-1874
07/05/1999
PMID: 10406657

Abstract

Sulfonamides - chemical synthesis Cricetinae Animals Models, Chemical Humans Indoles - chemical synthesis Adrenergic Agonists - chemical synthesis Adrenergic Agonists - pharmacology Indoles - pharmacology Structure-Activity Relationship Sulfonamides - pharmacology CHO Cells
A series of compounds possessing an N-substituted indoline-5-sulfonamide pharmacophore was prepared and evaluated for their human beta3 adrenergic receptor agonist activity. The SAR of a wide range of urea and heterocyclic substituents is discussed. 4-Octyl thiazole compound 8c was the most potent and selective compound in the series, with 2800-fold selectivity over beta1 binding and 1400-fold selectivity over beta2 binding.

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