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

H Wang, JA Robl, LG Hamann, L Simpkins…

Index: Wang, Haixia; Robl, Jeffrey A.; Hamann, Lawrence G.; Simpkins, Ligaya; Golla, Rajasree; Li, Yi-Xin; Seethala, Ramakrishna; Zvyaga, Tatyana; Gordon, David A.; Li, James J. Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 14 p. 4146 - 4149

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Citation Number: 16

Abstract

Abstract A series of pyridyl amide/sulfonamide inhibitors of 11β-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.

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