Novel phenyl-urea derivatives as dual-target ligands that can activate both GK and PPARγ

Lijian Zhang; Kang Tian; Yongqiang Li; Lei Lei; Aifang Qin; Lijuan Zhang; Hongrui Song; Lianchao Huo; Lijing Zhang; Xiaofeng Jin; Zhufang Shen; Zhiqiang Feng

doi:10.1016/j.apsb.2012.10.002

Acta Pharmaceutica Sinica B (Dec 2012)

Novel phenyl-urea derivatives as dual-target ligands that can activate both GK and PPARγ

Lijian Zhang,
Kang Tian,
Yongqiang Li,
Lei Lei,
Aifang Qin,
Lijuan Zhang,
Hongrui Song,
Lianchao Huo,
Lijing Zhang,
Xiaofeng Jin,
Zhufang Shen,
Zhiqiang Feng

Affiliations

Lijian Zhang: School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China
Kang Tian: School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China
Yongqiang Li: Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China
Lei Lei: Beijing Key Laboratory of Active Substance Discovery and Druggability Evaluation, Institute of Materia Medica,Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China
Aifang Qin: School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China
Lijuan Zhang: School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China
Hongrui Song: School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China
Lianchao Huo: Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China
Lijing Zhang: Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China
Xiaofeng Jin: Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China
Zhufang Shen: Beijing Key Laboratory of Active Substance Discovery and Druggability Evaluation, Institute of Materia Medica,Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China
Zhiqiang Feng: Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China

DOI: https://doi.org/10.1016/j.apsb.2012.10.002
Journal volume & issue: Vol. 2, no. 6
pp. 588 – 597

Abstract

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A series of novel phenyl-urea derivatives which can simultaneously activate glucokinase (GK) and peroxisome proliferator-activated receptor γ (PPARγ) was designed and prepared, and their activation of GK and PPARγ was evaluated. The structure–activity relationships of these compounds are also described. Three compounds showed potent ability to activate both GK and PPARγ. The possible binding mode of one of these compounds with GK and PPARγ were predicted by molecular docking simulation.

Published in Acta Pharmaceutica Sinica B

ISSN: 2211-3835 (Print); 2211-3843 (Online)
Publisher: Elsevier
Country of publisher: Netherlands
LCC subjects: Medicine: Therapeutics. Pharmacology
Website: http://www.journals.elsevier.com/acta-pharmaceutica-sinica-b

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