1610951-50-2Relevant academic research and scientific papers
Optimization of 1,2,4-triazolopyridines as inhibitors of human 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD-1)
Li, Jun,Kennedy, Lawrence J.,Wang, Haixia,Li, James J.,Walker, Steven J.,Hong, Zhenqiu,Oconnor, Stephen P.,Nayeem, Akbar,Camac, Daniel M.,Morin, Paul E.,Sheriff, Steven,Wang, Mengmeng,Harper, Timothy,Golla, Rajasree,Seethala, Ramakrishna,Harrity, Thomas,Ponticiello, Randolph P.,Morgan, Nathan N.,Taylor, Joseph R.,Zebo, Rachel,Gordon, David A.,Robl, Jeffrey A.
, p. 803 - 808 (2014/08/05)
Small alkyl groups and spirocyclic-aromatic rings directly attached to the left side and right side of the 1,2,4-triazolopyridines (TZP), respectively, were found to be potent and selective inhibitors of human 11β- hydroxysteroid dehydrogenase-type 1 (11β-HSD-1) enzyme. 3-(1-(4-Chlorophenyl)cyclopropyl)-8-cyclopropyl-[1,2,4]triazolo[4,3-a]pyridine (9f) was identified as a potent inhibitor of the 11β-HSD-1 enzyme with reduced Pregnane-X receptor (PXR) transactivation activity. The binding orientation of this TZP series was revealed by X-ray crystallography structure studies.
