N-(5-substituted thiazol-2-yl)-2-aryl-3-(tetrahydro-2H-pyran-4-yl) propanamides as glucokinase activators

Zhiqing Liu, Qingzhang Zhu, Fuying Li, Lina Zhang, Ying Leng, Ao Zhang

Research output: Contribution to journalArticle

9 Scopus citations

Abstract

A series of novel arylacetamides were designed to further explore the GK binding property at the aminothiazole C5 position. The C5-amide substituted aminothiazoles 7a-f generally displayed decreased potency, whereas most of the C5-triazole substituted aminothiazoles retained good GK potency. Triazole 15 with a hydroxyethyl side chain was the most potent among the current series possessing an EC50 value of 0.18 μM. Its R-enantiomer R-15 showed similar potency (0.22 μM) that deserves for further evaluation.

Original languageEnglish (US)
Pages (from-to)531-535
Number of pages5
JournalMedChemComm
Volume2
Issue number6
DOIs
StatePublished - Jun 1 2011

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ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Pharmacology
  • Pharmaceutical Science
  • Drug Discovery
  • Organic Chemistry

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