Add time:07/15/2019         Source:sciencedirect.com

A series of novel (4-piperidin-1-yl)-phenyl sulfonamides was prepared and evaluated for their biological activity on the human β3-adrenergic receptor (AR). Replacement of the 3,4-dihydroxyl group of the catechol moiety with 4-hydroxyl-3-methyl sulfonamide on the left-hand side of the compounds resulted in a number of potent full agonists at the β3 receptor. Modification of the right-hand side of the compounds by incorporation of a free carboxylic acid resulted in a few potent human β3 agonists with low affinities for β1- and β2-ARs. N-Alkyl substitution on the 4-piperidin-1-yl-phenylamine further increased the β3 potency while maintaining the selectivity. For example, sulfonamide 48 is a potent full β3 agonist (EC50=0.004 μM, IA=1.0) with >500-fold selectivity over β1- and β2-ARs.

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