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Molecules 2008, 13(4), 736-748; doi:10.3390/molecules13040736
Article

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

1,* , 2
,
1
,
1
 and
2
1 Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Mersin University, Mersin 33169, Turkey 2 Department of Bioanalytics, Institute for Pharmaceutical Chemistry, Heinrich-Heine University, Düsseldorf 40225, Germany
* Author to whom correspondence should be addressed.
Received: 12 February 2008 / Revised: 20 March 2008 / Accepted: 20 March 2008 / Published: 27 March 2008
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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. Hyaluronidase; benzimidazole; benzothiazole; indole; Morgan-Elson assay; stains-all assay and microwave irradiation.
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).
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Algul, O.; Kaessler, A.; Apcin, Y.; Yilmaz, A.; Jose, J. Comparative Studies on Conventional and Microwave Synthesis of Some Benzimidazole, Benzothiazole and Indole Derivatives and Testing on Inhibition of Hyaluronidase. Molecules 2008, 13, 736-748.

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