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Bioorg Med Chem Lett. 2010 May 1;20(9):2897-902. doi: 10.1016/j.bmcl.2010.03.032. Epub 2010 Mar 10.

The development and SAR of pyrrolidine carboxamide 11beta-HSD1 inhibitors.

Author information

1
Pfizer Global Research & Development, La Jolla Labs, 10770 Science Center Drive, San Diego, CA 92121, United States. henry.cheng@pfizer.com

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.

PMID:
20363126
DOI:
10.1016/j.bmcl.2010.03.032
[Indexed for MEDLINE]

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