Synthesis, potent anti-staphylococcal activity and QSARs of some novel 2-anilinobenzazoles

Oezden S., Atabey D., Yildiz S., Goeker H.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, cilt.43, sa.7, ss.1390-1402, 2008 (SCI-Expanded) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 43 Sayı: 7
  • Basım Tarihi: 2008
  • Doi Numarası: 10.1016/j.ejmech.2007.10.009
  • Dergi Adı: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus, Index Chemicus (IC)
  • Sayfa Sayıları: ss.1390-1402
  • Anahtar Kelimeler: anilinobenzimidazole, anilinobenzothiazole, anilinobenzoxazole, anti-staphy lococcal activity, k(w) capacity factors, QSAR, PERFORMANCE LIQUID-CHROMATOGRAPHY, ANTIMICROBIAL ACTIVITY, ACID-DERIVATIVES, LOG KW, LIPOPHILICITY, HYDROPHOBICITY, VALUES
  • Ankara Üniversitesi Adresli: Evet

Özet

Synthesis and anti-staphylococcal activity of a number of substituted 2-anilinobenzimidazoles, benzothiazoles and benzoxazoles are reported. The anti-staphylococcal activities were evaluated in standard in vitro MIC assay method. While anilinobenzimidazole derivatives 11-45 showed very potent anti-staphylococcal activities (greatest activity with an MIC value of 0.095 mu g/mL), none of the 2-anilinobenzothiazoles and benzoxazole derivatives exhibited inhibitory activity. QSAR analysis of the anilinobenzimidazoles was studied on the relationship between the anti-staphylococcal activity (MIC in mu g/ml) and extrapolated log k(w) values. (c) 2007 Elsevier Masson SAS. All rights reserved.