title: Discovery of cyclicsulfonamide derivatives as 11 beta-hydroxysteroid dehydrogenase 1 inhibitors.
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.
authors.affiliation: Department of Chemistry, Korea University, Seoul 121-742, Republic of Korea.
authors.forename: Se Hoan
authors.initials: SH
authors.lastname: Kim
authors.forename: Ravirala
authors.initials: R
authors.lastname: Ramu
authors.forename: Sung Wook
authors.initials: SW
authors.lastname: Kwon
authors.forename: Su-Hee
authors.initials: SH
authors.lastname: Lee
authors.forename: Chi Hyun
authors.initials: CH
authors.lastname: Kim
authors.forename: Seung Kyu
authors.initials: SK
authors.lastname: Kang
authors.forename: Sang Dal
authors.initials: SD
authors.lastname: Rhee
authors.forename: Myung Ae
authors.initials: MA
authors.lastname: Bae
authors.forename: Sung Hoon
authors.initials: SH
authors.lastname: Ahn
authors.forename: Duck Chan
authors.initials: DC
authors.lastname: Ha
authors.forename: Hyae Gyeong
authors.initials: HG
authors.lastname: Cheon
authors.forename: Ki Young
authors.initials: KY
authors.lastname: Kim
authors.forename: Jin Hee
authors.initials: JH
authors.lastname: Ahn
mesh_terms: D043205:11-beta-Hydroxysteroid Dehydrogenase Type 1 / Q000037:antagonists & inhibitors* / Q000378:metabolism; D000818:Animals; D002460:Cell Line; D055808:Drug Discovery / Q000379:methods*; D006801:Humans; D051379:Mice; D008861:Microsomes / Q000187:drug effects / Q000201:enzymology; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology
chemical_list: D013449:Sulfonamides; D043205:11-beta-Hydroxysteroid Dehydrogenase Type 1