title: Synthesis and biological evaluation of cyclic sulfamide derivatives as 11β-hydroxysteroid dehydrogenase 1 inhibitors.
abstract: A new series of cyclic sulfamide derivatives were synthesized and evaluated for their ability to inhibit 11β-HSD1. Among this series, 18e showed good in vitro activity toward human 11β-HSD1, selectivity against 11β-HSD2, microsomal stability, and pharmacokinetic and safety profiles (hERG, CYP, and acute toxicity). Additionally, 18e exhibited good in vivo efficacy in rat and monkey models.
authors.affiliation: Bio-Organic Science Division, Korea Research Institute of Chemical Technology , Yuseong-Gu, Daejeon, 305-600, Korea ; Department of Chemistry, Korea University , Sungbuk-gu, Seoul 136-701, Korea.
authors.forename: Se Hoan
authors.initials: SH
authors.lastname: Kim
authors.affiliation: Bio-Organic Science Division, Korea Research Institute of Chemical Technology , Yuseong-Gu, Daejeon, 305-600, Korea.
authors.forename: Ju Han
authors.initials: JH
authors.lastname: Bok
authors.affiliation: Bio-Organic Science Division, Korea Research Institute of Chemical Technology , Yuseong-Gu, Daejeon, 305-600, Korea ; Department of Chemistry, Korea University , Sungbuk-gu, Seoul 136-701, Korea.
authors.forename: Jae Hong
authors.initials: JH
authors.lastname: Lee
authors.affiliation: Bio-Organic Science Division, Korea Research Institute of Chemical Technology , Yuseong-Gu, Daejeon, 305-600, Korea ; Department of Chemistry, Korea University , Sungbuk-gu, Seoul 136-701, Korea.
authors.forename: Il Hyang
authors.initials: IH
authors.lastname: Kim
authors.affiliation: Bio-Organic Science Division, Korea Research Institute of Chemical Technology , Yuseong-Gu, Daejeon, 305-600, Korea ; Department of Chemistry, Korea University , Sungbuk-gu, Seoul 136-701, Korea.
authors.forename: Sung Wook
authors.initials: SW
authors.lastname: Kwon
authors.affiliation: Bio-Organic Science Division, Korea Research Institute of Chemical Technology , Yuseong-Gu, Daejeon, 305-600, Korea.
authors.forename: Gui Bin
authors.initials: GB
authors.lastname: Lee
authors.affiliation: Bio-Organic Science Division, Korea Research Institute of Chemical Technology , Yuseong-Gu, Daejeon, 305-600, Korea.
authors.forename: Seung Kyu
authors.initials: SK
authors.lastname: Kang
authors.affiliation: Bio-Organic Science Division, Korea Research Institute of Chemical Technology , Yuseong-Gu, Daejeon, 305-600, Korea.
authors.forename: Ji Seon
authors.initials: JS
authors.lastname: Park
authors.affiliation: Bio-Organic Science Division, Korea Research Institute of Chemical Technology , Yuseong-Gu, Daejeon, 305-600, Korea.
authors.forename: Won Hoon
authors.initials: WH
authors.lastname: Jung
authors.affiliation: Bio-Organic Science Division, Korea Research Institute of Chemical Technology , Yuseong-Gu, Daejeon, 305-600, Korea.
authors.forename: Hee Yeon
authors.initials: HY
authors.lastname: Kim
authors.affiliation: Bio-Organic Science Division, Korea Research Institute of Chemical Technology , Yuseong-Gu, Daejeon, 305-600, Korea.
authors.forename: Sang Dal
authors.initials: SD
authors.lastname: Rhee
authors.affiliation: Bio-Organic Science Division, Korea Research Institute of Chemical Technology , Yuseong-Gu, Daejeon, 305-600, Korea.
authors.forename: Sung Hoon
authors.initials: SH
authors.lastname: Ahn
authors.affiliation: Bio-Organic Science Division, Korea Research Institute of Chemical Technology , Yuseong-Gu, Daejeon, 305-600, Korea.
authors.forename: Myung Ae
authors.initials: MA
authors.lastname: Bae
authors.affiliation: Department of Chemistry, Korea University , Sungbuk-gu, Seoul 136-701, Korea.
authors.forename: Deok Chan
authors.initials: DC
authors.lastname: Ha
authors.affiliation: Bio-Organic Science Division, Korea Research Institute of Chemical Technology , Yuseong-Gu, Daejeon, 305-600, Korea.
authors.forename: Ki Young
authors.initials: KY
authors.lastname: Kim
authors.affiliation: Bio-Organic Science Division, Korea Research Institute of Chemical Technology , Yuseong-Gu, Daejeon, 305-600, Korea.
authors.forename: Jin Hee
authors.initials: JH
authors.lastname: Ahn
keywords: 11β-hydroxysteroid dehydrogenase type 1; adamantyl group; antidiabetic agents; cyclic sulfamide; diabetes