Generation of 3,8-substituted 1,2,4-triazolopyridines as potent inhibitors of human 11 beta-hydroxysteroid dehydrogenase type 1 (11 beta-HSD-1)

[摘要]：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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