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

Se Hoan Kim; Ravirala Ramu; Sung Wook Kwon; Su-Hee Lee; Chi Hyun Kim; Seung Kyu Kang; Sang Dal Rhee; Myung Ae Bae; Sung Hoon Ahn; Duck Chan Ha; Hyae Gyeong Cheon; Ki Young Kim; Jin Hee Ahn

doi:10.1016/j.bmcl.2009.12.035

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.

Authors

Se Hoan Kim¹, Ravirala Ramu, Sung Wook Kwon, Su-Hee Lee, Chi Hyun Kim, Seung Kyu Kang, Sang Dal Rhee, Myung Ae Bae, Sung Hoon Ahn, Duck Chan Ha, Hyae Gyeong Cheon, Ki Young Kim, Jin Hee Ahn

Affiliation

¹ Department of Chemistry, Korea University, Seoul 121-742, Republic of Korea.

PMID: 20045318
DOI: 10.1016/j.bmcl.2009.12.035

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.

Publication types

Comparative Study
Research Support, Non-U.S. Gov't

MeSH terms

11-beta-Hydroxysteroid Dehydrogenase Type 1 / antagonists & inhibitors*
11-beta-Hydroxysteroid Dehydrogenase Type 1 / metabolism
Animals
Cell Line
Drug Discovery / methods*
Humans
Mice
Microsomes / drug effects
Microsomes / enzymology
Sulfonamides / chemical synthesis*
Sulfonamides / metabolism
Sulfonamides / pharmacology

Substances

Sulfonamides
11-beta-Hydroxysteroid Dehydrogenase Type 1