Comparative studies on conventional and microwave synthesis of some benzimidazole, benzothiazole and indole derivatives and testing on inhibition of hyaluronidase


Creative Commons License

Algul Ö., Kaessler A., Apcin Y., Yilmaz A., Jose J.

MOLECULES, vol.13, no.4, pp.736-748, 2008 (SCI-Expanded) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 13 Issue: 4
  • Publication Date: 2008
  • Doi Number: 10.3390/molecules13040736
  • Journal Name: MOLECULES
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Page Numbers: pp.736-748
  • Keywords: hyaluronidase, benzimidazole, benzothiazole, indole, Morgan-Elson assay, stains-all assay and microwave irradiation, ENDOTHELIAL-CELL PROLIFERATION, DESIGN, LYASE, ACID
  • Erzincan Binali Yildirim University Affiliated: No

Abstract

We have synthesized twelve 2-substituted benzimidazole, benzothiazole and indole derivatives using on both microwave irradiation and conventional heating methods. The microwave method was observed to be more beneficial as it provides an increase of yield from 3% to 113% and a 95 to 98% reduction in time. All compounds were tested by a stains-all assay at pH 7 and by a Morgan-Elson assay at pH 3.5 for hyaluronidase inhibitory activity at a concentration of 100 mu M. The most potent compound was 2-(4-hydroxyphenyl)-3-phenylindole (12) with an IC50 value of 107 mu M at both pH 7 and 3.5.