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Comparative Studies on Conventional and Microwave Synthesis of Some Benzimidazole, Benzothiazole and Indole Derivatives and Testing on Inhibition of Hyaluronidase
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; in revised form: 20 March 2008 / Accepted: 20 March 2008 / Published: 27 March 2008
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.
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Cite This Article
MDPI and ACS Style
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.
AMA Style
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(4):736-748.
Chicago/Turabian Style
Algul, Oztekin; Kaessler, Andre; Apcin, Yagmur; Yilmaz, Akin; Jose, Joachim. 2008. "Comparative Studies on Conventional and Microwave Synthesis of Some Benzimidazole, Benzothiazole and Indole Derivatives and Testing on Inhibition of Hyaluronidase." Molecules 13, no. 4: 736-748.