The synthesis and the structure-activity relationships of some substituted benzoxazoles, oxazolo(4,5-b)pyridines, benzothiazoles and benzimidazoles as antimicrobial agents


Yalçın İ., Ören İ., Şener E., Akin A., Uçartürk N.

European Journal of Medicinal Chemistry, cilt.27, sa.4, ss.401-406, 1992 (SCI-Expanded) identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 27 Sayı: 4
  • Basım Tarihi: 1992
  • Doi Numarası: 10.1016/0223-5234(92)90154-s
  • Dergi Adı: European Journal of Medicinal Chemistry
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.401-406
  • Anahtar Kelimeler: antibacterial activity, antimycotic activity, benzimidazoles, benzothiazoles, benzoxazoles, oxazolo(4,5-b)pyridines, SAR
  • Ankara Üniversitesi Adresli: Evet

Özet

The synthesis of a new series of 2,5-disubstituted benzoxazoles 4a-f, 2-substituted oxazolo(4,5-b)pyridines 5a, b, benzothiazoles 6a, b and benzimidazoles 7a, b is described in order to determine their antimicrobial activities and feasible structure-activity relationships (SAR). The synthesized compounds were tested in vitro against 3 Gram-positive, 3 Gram-negative, and a fungus Candida albicans, 4b, 4e and 4f were found to be more active than the others against Klebsiella pneumoniae at a MIC value of 12.5 μg/ml. All the derivatives 4-7 exhibited significant antimycotic activity against C albicans. The antibacterial and antimycotic activities of 4-7 are also compared with several standard drugs. © 1992.