Benzamide derivatives as dual-action hypoglycemic agents that inhibit glycogen phosphorylase and activate glucokinase

Lei Zhang; Honglin Li; Qingzhang Zhu; Jun Liu; Ling Chen; Ying Leng; Hualiang Jiang; Hong Liu

doi:10.1016/j.bmc.2009.08.045

Benzamide derivatives as dual-action hypoglycemic agents that inhibit glycogen phosphorylase and activate glucokinase

Lei Zhang
, Honglin Li
, Qingzhang Zhu
, Jun Liu
, Ling Chen
, Ying Leng^*
, Hualiang Jiang
, Hong Liu

^*此作品的通讯作者

CAS - Shanghai Institute of Materia Medica
East China University of Science and Technology
China Pharmaceutical University

科研成果: 期刊稿件 › 文章 › 同行评审

36 引用（Scopus）

摘要

A series of benzamide derivatives which can simultaneously inhibit glycogen phosphorylase (GP) and activate glucokinase (GK) were prepared and evaluated. The structure-activity relationships (SAR) of these compounds were also presented. Among these, compounds 12, 13l, 13q, and 13v showed moderate activities towards both GK and GP. Compound 13h inhibited hLGP with an IC₅₀ of 8.95 μM and activated GK with an EC₅₀ of 1.87 μM. The possible binding modes of compounds 12, 13l, 13h, and 13q with GP and GK were also explored by molecular docking simulation.

源语言	英语
页（从-至）	7301-7312
页数	12
期刊	Bioorganic and Medicinal Chemistry
卷	17
期	20
DOI	https://doi.org/10.1016/j.bmc.2009.08.045
出版状态	已出版 - 15 10月 2009
已对外发布	是

联合国可持续发展目标

此成果有助于实现下列可持续发展目标：

可持续发展目标 3 良好健康与福祉

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10.1016/j.bmc.2009.08.045

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title = "Benzamide derivatives as dual-action hypoglycemic agents that inhibit glycogen phosphorylase and activate glucokinase",

abstract = "A series of benzamide derivatives which can simultaneously inhibit glycogen phosphorylase (GP) and activate glucokinase (GK) were prepared and evaluated. The structure-activity relationships (SAR) of these compounds were also presented. Among these, compounds 12, 13l, 13q, and 13v showed moderate activities towards both GK and GP. Compound 13h inhibited hLGP with an IC50 of 8.95 μM and activated GK with an EC50 of 1.87 μM. The possible binding modes of compounds 12, 13l, 13h, and 13q with GP and GK were also explored by molecular docking simulation.",

keywords = "Dual action, Glucokinase (GK) activators, Glycogen phosphorylase (GP) inhibitors, Type 2 diabetes",

author = "Lei Zhang and Honglin Li and Qingzhang Zhu and Jun Liu and Ling Chen and Ying Leng and Hualiang Jiang and Hong Liu",

year = "2009",

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doi = "10.1016/j.bmc.2009.08.045",

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TY - JOUR

T1 - Benzamide derivatives as dual-action hypoglycemic agents that inhibit glycogen phosphorylase and activate glucokinase

AU - Zhang, Lei

AU - Li, Honglin

AU - Zhu, Qingzhang

AU - Liu, Jun

AU - Chen, Ling

AU - Leng, Ying

AU - Jiang, Hualiang

AU - Liu, Hong

PY - 2009/10/15

Y1 - 2009/10/15

N2 - A series of benzamide derivatives which can simultaneously inhibit glycogen phosphorylase (GP) and activate glucokinase (GK) were prepared and evaluated. The structure-activity relationships (SAR) of these compounds were also presented. Among these, compounds 12, 13l, 13q, and 13v showed moderate activities towards both GK and GP. Compound 13h inhibited hLGP with an IC50 of 8.95 μM and activated GK with an EC50 of 1.87 μM. The possible binding modes of compounds 12, 13l, 13h, and 13q with GP and GK were also explored by molecular docking simulation.

AB - A series of benzamide derivatives which can simultaneously inhibit glycogen phosphorylase (GP) and activate glucokinase (GK) were prepared and evaluated. The structure-activity relationships (SAR) of these compounds were also presented. Among these, compounds 12, 13l, 13q, and 13v showed moderate activities towards both GK and GP. Compound 13h inhibited hLGP with an IC50 of 8.95 μM and activated GK with an EC50 of 1.87 μM. The possible binding modes of compounds 12, 13l, 13h, and 13q with GP and GK were also explored by molecular docking simulation.

KW - Dual action

KW - Glucokinase (GK) activators

KW - Glycogen phosphorylase (GP) inhibitors

KW - Type 2 diabetes

UR - https://www.scopus.com/pages/publications/71749089240

U2 - 10.1016/j.bmc.2009.08.045

DO - 10.1016/j.bmc.2009.08.045

M3 - 文章

C2 - 19758809

AN - SCOPUS:71749089240

SN - 0968-0896

VL - 17

SP - 7301

EP - 7312

JO - Bioorganic and Medicinal Chemistry

JF - Bioorganic and Medicinal Chemistry

IS - 20

ER -

Benzamide derivatives as dual-action hypoglycemic agents that inhibit glycogen phosphorylase and activate glucokinase

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