Optimization of 1,2,4-Triazolopyridines
as Inhibitors
of Human 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD-1)

Akbar Nayeem (1780588); Daniel
M. Camac (1780570); David
A. Gordon (1780564); Haixia Wang (173360); James
J. Li (1780576); Jeffrey A. Robl (278983); Joseph R. Taylor (278979); Jun Li (6494); Lawrence
J. Kennedy (1780567); Mengmeng Wang (540017); Nathan N. Morgan (1780579); Paul E. Morin (1629814); Rachel Zebo (1745224); Rajasree Golla (1780585); Ramakrishna Seethala (1780555); Randolph
P. Ponticiello (1780561); Stephen P. O’Connor (1780582); Steven J. Walker (1780573); Steven Sheriff (1601854); Thomas Harrity (1780558); Timothy Harper (1601815); Zhenqiu Hong (1745164)

Optimization of 1,2,4-Triazolopyridines as Inhibitors of Human 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD-1)

Abstract

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-<i>a</i>]pyridine (<b>9f</b>) 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

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Last time updated on 12/02/2018