Comparative Studies on Conventional and Microwave Synthesis of Some Benzimidazole, Benzothiazole and Indole Derivatives and Testing on Inhibition of Hyaluronidase

Abstract

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

Keywords

• Hyaluronidase
• benzimidazole
• benzothiazole
• indole
• Morgan-Elson assay
• stains-all assay and microwave irradiation.