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

Research output: Contribution to journalArticlepeer-review

29 Scopus citations

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.

Original languageEnglish (US)
Pages (from-to)7301-7312
Number of pages12
JournalBioorganic and Medicinal Chemistry
Volume17
Issue number20
DOIs
StatePublished - Oct 15 2009
Externally publishedYes

Keywords

  • Dual action
  • Glucokinase (GK) activators
  • Glycogen phosphorylase (GP) inhibitors
  • Type 2 diabetes

ASJC Scopus subject areas

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

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