Design, synthesis and biological evaluation of GY3-based derivatives for anti-type 2 diabetes activity

Bioorg Med Chem Lett. 2015 Apr 1;25(7):1500-5. doi: 10.1016/j.bmcl.2015.02.021. Epub 2015 Feb 18.

Abstract

A series of indole carboxylic acid derivatives were designed and synthesized. Their anti-type 2 diabetes activity was evaluated in HepG2 cell and db/db mice. The results showed that compounds 8c, 17a, 17b, 15a and 15b could significantly increase glucose consumption in HepG2 cell. Furthermore, compound 8c was able to lower the blood glucose level and induce less weight gain in db/db mice.

Keywords: Anti-type 2 diabetes activity; Design; Indole carboxylic acid derivatives; Synthesis.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Diabetes Mellitus, Experimental / drug therapy*
  • Diabetes Mellitus, Type 2 / drug therapy*
  • Drug Design*
  • Hep G2 Cells
  • Humans
  • Indoleacetic Acids / chemical synthesis
  • Indoleacetic Acids / chemistry
  • Indoleacetic Acids / pharmacology*
  • Mice
  • Mice, Mutant Strains
  • Molecular Structure

Substances

  • 1-(4-chlorobenzoyl)-5-hydroxy-2-methyl-3-indoleacetic acid
  • Indoleacetic Acids