| Literature DB >> 20363126 |
Hengmiao Cheng1, Jacqui Hoffman, Phuong Le, Sajiv K Nair, Stephan Cripps, Jean Matthews, Christopher Smith, Michele Yang, Stan Kupchinsky, Klaus Dress, Martin Edwards, Bridget Cole, Evan Walters, Christine Loh, Jacques Ermolieff, Andrea Fanjul, Ganesh B Bhat, Jocelyn Herrera, Tom Pauly, Natilie Hosea, Genevieve Paderes, Paul Rejto.
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. 2010 Elsevier Ltd. All rights reserved.Entities:
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Year: 2010 PMID： 20363126 DOI： 10.1016/j.bmcl.2010.03.032
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823