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Letters in Drug Design & Discovery


ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

A Microplate based Screening of Benzimidazole Derivatives on Hyaluronidase Inhibition at PH 7 and 3.5

Author(s): Andre Kaessler, Oztekin Algul and Joachim Jose

Volume 4 , Issue 8 , 2007

Page: [562 - 569] Pages: 8

DOI: 10.2174/157018007782794491

Price: $65


Two microplate assays for inhibitor testing were established and used to identify new hyaluronidase inhibitors from a series of benzimidazole derivatives. In vitro assays were performed at pH 7 using a “stains-all” based assay and at pH 3.5 using a Morgan-Elson assay. Twelve benzimidazole derivatives were synthesized and tested on hyaluronidase inhibition at a concentration of 100 μM and IC50 values of the compounds with an inhibition of more than 50 % were determined. The most potent compound was 4b (Di(1H-benzo[d]imidazol-2-yl)methane) with an IC50 value of 78 μM at pH 7 and 72 μM at pH 3.5, respectively.

Keywords: Hyaluronic acid, Hyaluronidase, Benzimidazoles, Morgan-Elson, Stains-all

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