Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 21, Issue 14, Pages 4146-4149Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2011.05.101
Keywords
Type 2 diabetes; 11 beta-HSD-1 inhibitors; Triazolopyridine; PXR
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A series of pyridyl amide/sulfonamide inhibitors of 11 beta-HSD-1 were modified to incorporate a novel 1,2,4-triazolopyridine scaffold. Optimization of substituents at the 3 and 8 position of the TZP core, with a special focus on enhancing metabolic stability, resulted in the identification of compound 38 as a potent and metabolically stable inhibitor of the enzyme. (C) 2011 Elsevier Ltd. All rights reserved.
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