1026309-05-6Relevant articles and documents
Generation of 3,8-substituted 1,2,4-triazolopyridines as potent inhibitors of human 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD-1)
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.
, p. 4146 - 4149 (2011/08/10)
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.