Synthesis and structure-activity relationships of new antimicrobial active multisubstituted benzazole derivatives

Yildiz-Oren İ., Yalcin I., Aki-Sener E., Ucarturk N.

European Journal of Medicinal Chemistry, cilt.39, sa.3, ss.291-298, 2004 (SCI-Expanded) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 39 Sayı: 3
  • Basım Tarihi: 2004
  • Doi Numarası: 10.1016/j.ejmech.2003.11.014
  • Dergi Adı: European Journal of Medicinal Chemistry
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.291-298
  • Anahtar Kelimeler: synthesis, antimicrobial activity, benzoxazole, benzimidazole, benzothiazole, HIV-1 REVERSE-TRANSCRIPTASE, CYTOTOXIC METABOLITE, ANTITUMOR BENZOTHIAZOLES, MICROBIOLOGICAL ACTIVITY, BENZOXAZOLES, BENZIMIDAZOLES, UK-1, OXAZOLO(4,5-B)PYRIDINES, ZIDOVUDINE, RESISTANCE
  • Ankara Üniversitesi Adresli: Evet

Özet

A series of multisubstituted benzoxazoles, benzimidazoles, and benzothiazoles (5-7) as non-nucleoside fused isosteric heterocyclic compounds was synthesized and tested for their antibacterial activities against various Gram-positive and Gram-negative bacteria and antifungal activity against the fungus Candida albicans. Microbiological results indicated that the synthesized compounds possessed a broad spectrum of activity against the tested microorganisms at MIC values between 100 and 3.12 μg/ml. Structure-activity relationships (SAR) studies revealed that benzothiazole ring system enhanced the antimicrobial activity against Staphylococcus aureus. In these sets of non-nucleoside fused heterocyclic compounds electron withdrawing groups at position 5 of the benzazoles increased the activity against C. albicans. © 2003 Elsevier SAS. All rights reserved.