Identification of Cyclicsulfonamide Derivatives with an Acetamide Group as 11β-Hydroxysteroid Dehydrogenase 1 Inhibitors
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概要
- 論文の詳細を見る
In the continuation of our 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor research, cyclic sulfonamide derivatives with an acetamide group at the 2-position were synthesized and evaluated for their abilities to inhibit 11β-HSD1. Among this series, Compound 34 showed good in vitro activity toward human 11β-HSD1, selectivity against 11β-HSD2, microsomal stability, good pharmacokinetic and safety profiles human ether-a-go-go related gene (hERG and cytochrome P450 (CYP)). Also, a docking study explained the activity difference between human and mouse 11β-HSD1.
著者
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Kim Se
Department of Radiology, Seoul National University Hospital
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LEE Jae
Department of Metallurgy, The University of Tokyo
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Kwon Sung
Department of Chemistry, Korea University
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Chu So
Drug Discovery Division, Korea Research Institute of Chemical Technology
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Narsaiah Banda
Drug Discovery Division, Korea Research Institute of Chemical Technology
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Kim Chi
Drug Discovery Division, Korea Research Institute of Chemical Technology
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Kang Seung
Drug Discovery Division, Korea Research Institute of Chemical Technology
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Kang Nam
Drug Discovery Division, Korea Research Institute of Chemical Technology
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Rhee Sang
Drug Discovery Division, Korea Research Institute of Chemical Technology
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Bae Myung
Drug Discovery Division, Korea Research Institute of Chemical Technology
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Ahn Sung
Drug Discovery Division, Korea Research Institute of Chemical Technology
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Ha Duck
Department of Chemistry, Korea University
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Kim Ki
Drug Discovery Division, Korea Research Institute of Chemical Technology
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Ahn Jin
Drug Discovery Division, Korea Research Institute of Chemical Technology
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Kim Se
Department Of Anatomy College Of Veterinary Medicine Chonnam National University
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Ahn Jin
Drug Discovery Division Korea Research Institute Of Chemical Technology
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Lee Jae
Department Of Acupuncture & Moxibustion College Of Oriental Medicine
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Kang Seung
Drug Discovery Division Korea Research Institute Of Chemical Technology
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Kim Se
Department of Chemistry, Korea University
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