4-(Phenylsulfonamidomethyl)benzamides as potent and selective inhibitors of the 11β-hydroxysteroid dehydrogenase type 1 with efficacy in diabetic ob/ob mice

Xu Zhang; Zhou Zhou; Huaiyu Yang; Junhua Chen; Ying Feng; Lili Du; Ying Leng; Jianhua Shen

doi:10.1016/j.bmcl.2009.05.033

4-(Phenylsulfonamidomethyl)benzamides as potent and selective inhibitors of the 11β-hydroxysteroid dehydrogenase type 1 with efficacy in diabetic ob/ob mice

Xu Zhang
, Zhou Zhou
, Huaiyu Yang
, Junhua Chen
, Ying Feng
, Lili Du
, Ying Leng^*
, Jianhua Shen

^*Corresponding author for this work

CAS - Shanghai Institute of Materia Medica

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

17 Scopus citations

Abstract

Selective inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) have considerable potential as treatments for type 2 diabetes. Presented herein are the syntheses, structure-activity relationships, and efficacy evaluation of 4-(phenylsulfonamidomethyl)benzamides as 11β-HSD1 inhibitors. Through modification of our initial lead 5, we have identified potent and selective 11β-HSD1 inhibitors, such as 11n, which demonstrated improved glycemic control, decreased serum lipids, and enhanced insulin sensitivity when dosed ip in diabetic ob/ob mice. Crown

Original language	English
Pages (from-to)	4455-4458
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	19
Issue number	15
DOIs	https://doi.org/10.1016/j.bmcl.2009.05.033
State	Published - 1 Aug 2009
Externally published	Yes

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

SDG 3 Good Health and Well-being

Keywords

11β-HSD1 inhibitors
4-(Phenylsulfonamidomethyl)benzamide
Type 2 diabetes

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10.1016/j.bmcl.2009.05.033

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title = "4-(Phenylsulfonamidomethyl)benzamides as potent and selective inhibitors of the 11β-hydroxysteroid dehydrogenase type 1 with efficacy in diabetic ob/ob mice",

abstract = "Selective inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) have considerable potential as treatments for type 2 diabetes. Presented herein are the syntheses, structure-activity relationships, and efficacy evaluation of 4-(phenylsulfonamidomethyl)benzamides as 11β-HSD1 inhibitors. Through modification of our initial lead 5, we have identified potent and selective 11β-HSD1 inhibitors, such as 11n, which demonstrated improved glycemic control, decreased serum lipids, and enhanced insulin sensitivity when dosed ip in diabetic ob/ob mice. Crown",

keywords = "11β-HSD1 inhibitors, 4-(Phenylsulfonamidomethyl)benzamide, Type 2 diabetes",

author = "Xu Zhang and Zhou Zhou and Huaiyu Yang and Junhua Chen and Ying Feng and Lili Du and Ying Leng and Jianhua Shen",

year = "2009",

month = aug,

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doi = "10.1016/j.bmcl.2009.05.033",

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TY - JOUR

T1 - 4-(Phenylsulfonamidomethyl)benzamides as potent and selective inhibitors of the 11β-hydroxysteroid dehydrogenase type 1 with efficacy in diabetic ob/ob mice

AU - Zhang, Xu

AU - Zhou, Zhou

AU - Yang, Huaiyu

AU - Chen, Junhua

AU - Feng, Ying

AU - Du, Lili

AU - Leng, Ying

AU - Shen, Jianhua

PY - 2009/8/1

Y1 - 2009/8/1

N2 - Selective inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) have considerable potential as treatments for type 2 diabetes. Presented herein are the syntheses, structure-activity relationships, and efficacy evaluation of 4-(phenylsulfonamidomethyl)benzamides as 11β-HSD1 inhibitors. Through modification of our initial lead 5, we have identified potent and selective 11β-HSD1 inhibitors, such as 11n, which demonstrated improved glycemic control, decreased serum lipids, and enhanced insulin sensitivity when dosed ip in diabetic ob/ob mice. Crown

AB - Selective inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) have considerable potential as treatments for type 2 diabetes. Presented herein are the syntheses, structure-activity relationships, and efficacy evaluation of 4-(phenylsulfonamidomethyl)benzamides as 11β-HSD1 inhibitors. Through modification of our initial lead 5, we have identified potent and selective 11β-HSD1 inhibitors, such as 11n, which demonstrated improved glycemic control, decreased serum lipids, and enhanced insulin sensitivity when dosed ip in diabetic ob/ob mice. Crown

KW - 11β-HSD1 inhibitors

KW - 4-(Phenylsulfonamidomethyl)benzamide

KW - Type 2 diabetes

UR - https://www.scopus.com/pages/publications/67650178262

U2 - 10.1016/j.bmcl.2009.05.033

DO - 10.1016/j.bmcl.2009.05.033

M3 - 文章

C2 - 19564108

AN - SCOPUS:67650178262

SN - 0960-894X

VL - 19

SP - 4455

EP - 4458

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 15

ER -

4-(Phenylsulfonamidomethyl)benzamides as potent and selective inhibitors of the 11β-hydroxysteroid dehydrogenase type 1 with efficacy in diabetic ob/ob mice

Abstract

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Keywords

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