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

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

doi:10.1016/j.bmcl.2009.12.035

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

Kim, Se Hoan;
Ramu, Ravirala;
Kwon, Sung Wook;
Lee, Su-Hee;
Kim, Chi Hyun;
... Ahn, Sung Hoon;
외 7명

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41

초록

A new series of cyclic sulfonamide derivatives was synthesized and evaluated for their ability to inhibit 11 beta-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 11 beta-HSD2. (C) 2009 Elsevier Ltd. All rights reserved.

키워드

11 beta-Hydroxysteroid dehydrogenase 1; Cyclic sulfonamide; Diabetes; Inhibitor; SELECTIVE INHIBITORS; METABOLIC SYNDROME; VISCERAL OBESITY; TYPE-1; MICE; POTENT

제목: Discovery of cyclicsulfonamide derivatives as 11β-hydroxysteroid dehydrogenase 1 inhibitors

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

DOI: 10.1016/j.bmcl.2009.12.035

발행일: 2010-02-01

유형: Article

저널명: Bioorganic & Medicinal Chemistry Letters

권: 20

호: 3

페이지: 1065 ~ 1069

언어: ENG

출판사: PERGAMON-ELSEVIER SCIENCE LTD

발행국가: 영국

분량: 5 페이지

ISSN: E 1464-3405
P 0960-894X