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J Med Chem. 2001 Apr 26;44(9):1456-66.

(4-Piperidin-1-yl)phenyl amides: potent and selective human beta(3) agonists.

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  • 1Chemical Sciences and Cardiovascular/Metabolic Diseases Research, Wyeth-Ayerst Research, Pearl River, New York 10965, USA. hub@war.wyeth.com


In search of potent and selective human beta(3) agonists as potential drugs for the treatment of human obesity and type II diabetes, a series of (4-piperidin-1-yl)phenyl amides was prepared and evaluated for their biological activity on the human beta(3)-adrenergic receptor. The leucine derivative 26e and the reverse amide 33b were found to be the two most potent and selective compounds in this study. With EC(50) values of 0.008 and 0.009 microM, respectively, at the beta(3) receptor, nearly completely abolished intrinsic activity at either the beta(1) or beta(2) receptor, and significant thermogenesis effects on human beta(3)-adrenergic receptor transgenic mice, 26e and33b are among the most potent and selective human beta(3) agonists known to date.

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