Synthesis of azaisoflavones and their inhibitory activities of NO production in activated microglia

Bioorg Med Chem Lett. 2008 Jul 15;18(14):4092-4. doi: 10.1016/j.bmcl.2008.05.106. Epub 2008 Jun 13.

Abstract

A series of azaisoflavones were synthesized and their biological activities were evaluated for nitric oxide (NO) production and inducible NO synthase (iNOS) expression in BV-2 microglia cell lines. Among these compounds, compound 8d was the most potent with IC(50) 7.83 microM for inhibition of NO production. Also, compound 8d inhibited expression of iNOS in LPS-induced BV2 cells. This result suggests that compound 8d inhibited the production of NO by suppressing the expression of iNOS.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cell Line
  • Chemistry, Pharmaceutical / methods
  • Drug Design
  • Inhibitory Concentration 50
  • Isoflavones / chemistry*
  • Mice
  • Microglia / drug effects
  • Microglia / metabolism*
  • Models, Chemical
  • Nitric Oxide / chemistry*
  • Nitric Oxide Synthase Type II / metabolism*
  • Quinolones / chemistry
  • Temperature
  • Tetrazolium Salts / pharmacology
  • Thiazoles / pharmacology

Substances

  • Isoflavones
  • Quinolones
  • Tetrazolium Salts
  • Thiazoles
  • Nitric Oxide
  • Nitric Oxide Synthase Type II
  • thiazolyl blue