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The development and SAR of pyrrolidine carboxamide 11beta-HSD1 inhibitors.
Cheng, Hengmiao; Hoffman, Jacqui; Le, Phuong; Nair, Sajiv K; Cripps, Stephan; Matthews, Jean; Smith, Christopher; Yang, Michele; Kupchinsky, Stan; Dress, Klaus; Edwards, Martin; Cole, Bridget; Walters, Evan; Loh, Christine; Ermolieff, Jacques; Fanjul, Andrea; Bhat, Ganesh B; Herrera, Jocelyn; Pauly, Tom; Hosea, Natilie; Paderes, Genevieve; Rejto, Paul.
Bioorg Med Chem Lett ; 20(9): 2897-902, 2010 May 01.
Article in English | MEDLINE | ID: mdl-20363126

ABSTRACT

The design and development of a series of highly selective pyrrolidine carboxamide 11beta-HSD1 inhibitors are described. These compounds including PF-877423 demonstrated potent in vitro activity against both human and mouse 11beta-HSD1 enzymes. In an in vivo assay, PF-877423 inhibited the conversion of cortisone to cortisol. Structure guided optimization effort yielded potent and stable 11beta-HSD1 selective inhibitor 42.


Subject(s)
11-beta-Hydroxysteroid Dehydrogenase Type 1/antagonists & inhibitors , Adamantane/analogs & derivatives , Amides/chemistry , Enzyme Inhibitors/chemistry , Hypoglycemic Agents/chemistry , Pyrrolidines/chemistry , 11-beta-Hydroxysteroid Dehydrogenase Type 1/metabolism , Adamantane/chemical synthesis , Adamantane/chemistry , Adamantane/pharmacology , Amides/chemical synthesis , Amides/pharmacology , Animals , Enzyme Inhibitors/chemical synthesis , Enzyme Inhibitors/pharmacology , Guinea Pigs , Humans , Hypoglycemic Agents/chemical synthesis , Hypoglycemic Agents/pharmacology , Mice , Microsomes, Liver/metabolism , Pyrrolidines/chemical synthesis , Pyrrolidines/pharmacology , Structure-Activity Relationship
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