A microplate based screening of benzimidazole derivatives on hyaluronidase inhibition at PH 7 and 3.5

Kaessler A., Algul Ö., Jose J.

LETTERS IN DRUG DESIGN & DISCOVERY, cilt.4, sa.8, ss.562-569, 2007 (SCI-Expanded) identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 4 Sayı: 8
  • Basım Tarihi: 2007
  • Doi Numarası: 10.2174/157018007782794491
  • Dergi Adı: LETTERS IN DRUG DESIGN & DISCOVERY
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.562-569
  • Anahtar Kelimeler: hyaluronic acid, hyaluronidase, benzimidazoles, Morgan-Elson, stains-all, ENDOTHELIAL-CELL PROLIFERATION, PLATINUM(II) COMPLEXES, BINDING, ASSAY, EXPRESSION, ACID, DYE
  • Erzincan Binali Yıldırım Üniversitesi Adresli: Hayır

Özet

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 mu M 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 mu M at pH 7 and 72 mu M at pH 3.5, respectively.