Comparative studies on conventional and microwave synthesis of some benzimidazole, benzothiazole and indole derivatives and testing on inhibition of hyaluronidase

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Algul Ö., Kaessler A., Apcin Y., Yilmaz A., Jose J.

MOLECULES, cilt.13, sa.4, ss.736-748, 2008 (SCI-Expanded) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 13 Sayı: 4
  • Basım Tarihi: 2008
  • Doi Numarası: 10.3390/molecules13040736
  • Dergi Adı: MOLECULES
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.736-748
  • Anahtar Kelimeler: hyaluronidase, benzimidazole, benzothiazole, indole, Morgan-Elson assay, stains-all assay and microwave irradiation, ENDOTHELIAL-CELL PROLIFERATION, DESIGN, LYASE, ACID
  • Erzincan Binali Yıldırım Üniversitesi Adresli: Hayır

Özet

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 mu M. The most potent compound was 2-(4-hydroxyphenyl)-3-phenylindole (12) with an IC50 value of 107 mu M at both pH 7 and 3.5.