Generation of 3,8-substituted 1,2,4-triazolopyridines as potent inhibitors of human 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD-1)
2011
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.
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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