Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 19, Issue 15, Pages 4325-4329Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.05.069
Keywords
NPY; Y1 Receptor; Antagonist; Anti-obesity; Food intake inhibition; 2,4-Diaminopyridine derivatives
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The synthesis and evaluation of a series of 2,4-diaminopyridine-based neuropeptide Y Y1 ( NPY Y1) receptor antagonists are described. Compound 1 was previously reported by our laboratory to be a potent and selective Y1 antagonist; however, 1 was also found to have potent hERG inhibitory activity. The main focus of this communication is structure-activity relationship development aimed at eliminating the hERG activity of 1. This resulted in the identification of compound 3d as a potent and selective NPY Y1 antagonist with reduced hERG liability. (C) 2009 Elsevier Ltd. All rights reserved.
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