Bioorg Med Chem Lett. 2010 Feb 1;20(3):1065-9. Epub 2009 Dec 11.

Discovery of cyclicsulfonamide derivatives as 11 beta-hydroxysteroid dehydrogenase 1 inhibitors.

Kim SH, Ramu R, Kwon SW, Lee SH, Kim CH, Kang SK, Rhee SD, Bae MA, Ahn SH, Ha DC, Cheon HG, Kim KY, Ahn JH.

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Department of Chemistry, Korea University, Seoul 121-742, Republic of Korea.

Abstract

A new series of cyclic sulfonamide derivatives was synthesized and evaluated for their ability to inhibit 11beta-HSD1. Cyclic sulfonamides with phenylacetyl substituents at the 2-position showed nanomolar inhibitory activities. Among them, compound 4e exhibited a good in vitro inhibitory activity and selectivity toward human 11beta-HSD2.

PMID:: 20045318; [PubMed - indexed for MEDLINE]

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