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

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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

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

Bioorg Med Chem Lett. 2010 Feb 1;20(3):1065-9. doi: 10.1016/j.bmcl.2009.12.035. Epub 2009 Dec 11.

PubMed ID

20045318 [ View in PubMed

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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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Carbenoxolone	Corticosteroid 11-beta-dehydrogenase isozyme 1	IC 50 (nM)	500	N/A	N/A	Details