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, vol.27, no.4, pp.401-406, 1992 (SCI-Expanded) identifier

  • Publication Type: Article / Article
  • Volume: 27 Issue: 4
  • Publication Date: 1992
  • Doi Number: 10.1016/0223-5234(92)90154-s
  • Journal Name: European Journal of Medicinal Chemistry
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Page Numbers: pp.401-406
  • Keywords: antibacterial activity, antimycotic activity, benzimidazoles, benzothiazoles, benzoxazoles, oxazolo(4,5-b)pyridines, SAR
  • Ankara University Affiliated: Yes

Abstract

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.