Discovery of cyclicsulfonamide derivatives as 11β-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 11β-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

Research output: Contribution to journal › Article › peer-review

37 Citations (Scopus)

Abstract

A new series of cyclic sulfonamide derivatives was synthesized and evaluated for their ability to inhibit 11β-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 11β-HSD2.

Original language	English
Pages (from-to)	1065-1069
Number of pages	5
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	20
Issue number	3
DOIs	https://doi.org/10.1016/j.bmcl.2009.12.035
Publication status	Published - 2010 Feb 1

Bibliographical note

Funding Information:
This research was supported by the Center for Biological Modulators of the 21st Century Frontier R&D Program , Ministry of Education, Science and Technology, Korea .

Keywords

11β-Hydroxysteroid dehydrogenase 1
Cyclic sulfonamide
Diabetes
Inhibitor

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.1016/j.bmcl.2009.12.035

Cite this

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title = "Discovery of cyclicsulfonamide derivatives as 11β-hydroxysteroid dehydrogenase 1 inhibitors",

abstract = "A new series of cyclic sulfonamide derivatives was synthesized and evaluated for their ability to inhibit 11β-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 11β-HSD2.",

keywords = "11β-Hydroxysteroid dehydrogenase 1, Cyclic sulfonamide, Diabetes, Inhibitor",

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

note = "Funding Information: This research was supported by the Center for Biological Modulators of the 21st Century Frontier R&D Program , Ministry of Education, Science and Technology, Korea . ",

year = "2010",

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day = "1",

doi = "10.1016/j.bmcl.2009.12.035",

language = "English",

volume = "20",

pages = "1065--1069",

journal = "Bioorganic and Medicinal Chemistry Letters",

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TY - JOUR

T1 - Discovery of cyclicsulfonamide derivatives as 11β-hydroxysteroid dehydrogenase 1 inhibitors

AU - Kim, Se Hoan

AU - Ramu, Ravirala

AU - Kwon, Sung Wook

AU - Lee, Su Hee

AU - Kim, Chi Hyun

AU - Kang, Seung Kyu

AU - Rhee, Sang Dal

AU - Bae, Myung Ae

AU - Ahn, Sung Hoon

AU - Ha, Duck Chan

AU - Cheon, Hyae Gyeong

AU - Kim, Ki Young

AU - Ahn, Jin Hee

N1 - Funding Information: This research was supported by the Center for Biological Modulators of the 21st Century Frontier R&D Program , Ministry of Education, Science and Technology, Korea .

PY - 2010/2/1

Y1 - 2010/2/1

N2 - A new series of cyclic sulfonamide derivatives was synthesized and evaluated for their ability to inhibit 11β-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 11β-HSD2.

AB - A new series of cyclic sulfonamide derivatives was synthesized and evaluated for their ability to inhibit 11β-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 11β-HSD2.

KW - 11β-Hydroxysteroid dehydrogenase 1

KW - Cyclic sulfonamide

KW - Diabetes

KW - Inhibitor

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U2 - 10.1016/j.bmcl.2009.12.035

DO - 10.1016/j.bmcl.2009.12.035

M3 - Article

C2 - 20045318

AN - SCOPUS:74049154856

SN - 0960-894X

VL - 20

SP - 1065

EP - 1069

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 3

ER -

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

Abstract

Bibliographical note

Keywords

ASJC Scopus subject areas

UN SDGs

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