Discovery of camphor-derived pyrazolones as 11β-hydroxysteroid dehydrogenase type 1 inhibitors.
Basic Information
ID: ALA3286136
Journal: Bioorg Med Chem Lett
Title: Discovery of camphor-derived pyrazolones as 11β-hydroxysteroid dehydrogenase type 1 inhibitors.
Authors: Gillespie P, Pietranico-Cole S, Myers M, Bilotta JA, Conde-Knape K, Fotouhi N, Goodnow RA, Guertin KR, Hamilton MM, Haynes NE, Liu B, Qi L, Ren Y, Scott NR, So SS, Spence C, Taub R, Thakkar K, Tilley JW, Zwingelstein C.
Abstract: Starting from screening hit, (4S,7R)-1,7,8,8-tetramethyl-2-phenyl-1,2,4,5,6,7-hexahydro-4,7-methano-indazol-3-one (7), we optimized the potency and pharmacokinetic properties. This led to the identification of compounds with good in vivo activity in a mouse pharmacodynamic model of inhibition of 11βHSD1.
CiteXplore: 24815509
DOI: 10.1016/j.bmcl.2014.04.049
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