- Generation of 3,8-substituted 1,2,4-triazolopyridines as potent inhibitors of human 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD-1).
Generation of 3,8-substituted 1,2,4-triazolopyridines as potent inhibitors of human 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD-1).
Bioorganic & medicinal chemistry letters (2011-06-22)
Haixia Wang, Jeffrey A Robl, Lawrence G Hamann, Ligaya Simpkins, Rajasree Golla, Yi-Xin Li, Ramakrishna Seethala, Tatyana Zvyaga, David A Gordon, James J Li
PMID21689935
摘要
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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