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

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

Volume: 4 Issue: 8

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

Affiliation:

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

Abstract: 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.

Cite this article as:

Kaessler Andre, Algul Oztekin and Jose Joachim, A Microplate based Screening of Benzimidazole Derivatives on Hyaluronidase Inhibition at PH 7 and 3.5, Letters in Drug Design & Discovery 2007; 4 (8) . https://dx.doi.org/10.2174/157018007782794491