Potent, Elective Human Beta3 Adrenergic Receptor Agonists Containing a Substituted Indoline-5-sulfonamide Pharmacophore

Overview

Journal Bioorg Med Chem Lett

Specialty Biochemistry

Date 1999 Jul 16

PMID 10406657

Citations 4

Authors

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

A E Weber

Affiliations

Soon will be listed here.

Abstract

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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