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Comparative Study
. 2008 Mar 27;13(4):736-48.
doi: 10.3390/molecules13040736.

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

Oztekin Algul  1 , Andre Kaessler, Yagmur Apcin, Akin Yilmaz, Joachim Jose
Affiliations
Comparative Study

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

Oztekin Algul et al. Molecules. .

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 microM. The most potent compound was 2-(4-hydroxyphenyl)-3-phenylindole (12) with an IC(50) value of 107 microM at both pH 7 and 3.5.

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Figures

Scheme 1
Scheme 1
The syntheses of compounds 1-12.
See this image and copyright information in PMC

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