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

Molecules

Oztekin Algul²  Andre Kaessler¹  Yagmur Apcin²  Akin Yilmaz² 

[1] Bioanalytics, Institute of Pharmaceutical and Medicinal Chemistry, Heinrich-Heine-University, Düsseldorf 40225, Germany; E-mails:;Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Mersin University, Mersin 33169, Turkey; Tel: [phone]; Fax: [phone]; E-mails:

关键词: Hyaluronidase;    benzimidazole;    benzothiazole;    indole;    Morgan-Elson assay;    stains-all assay;    microwave irradiation;   

DOI  :  10.3390/molecules13040736

来源: mdpi

【 摘 要 】

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 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.

【 授权许可】

Unknown   
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