Format

Send to

Choose Destination
Bioorg Med Chem Lett. 2010 Dec 1;20(23):7071-5. doi: 10.1016/j.bmcl.2010.09.097. Epub 2010 Sep 29.

The synthesis and SAR of novel diarylsulfone 11β-HSD1 inhibitors.

Author information

1
Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, USA. xueleiy@amgen.com

Abstract

In this communication, human 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitory activities of a novel series of diarylsulfones are described. Optimization of this series resulted in several highly potent 11β-HSD1 inhibitors with excellent pharmacokinetic (PK) properties. Compound (S)-25 showed excellent efficacy in a non-human primate ex vivo pharmacodynamic model.

PMID:
20971000
DOI:
10.1016/j.bmcl.2010.09.097
[Indexed for MEDLINE]

Supplemental Content

Full text links

Icon for Elsevier Science
Loading ...
Support Center