Novel Benzoxazoles: Synthesis and Antibacterial, Antifungal, and Antitubercular Activity against Antibiotic-Resistant and -Sensitive Microbes

Arisoy M., Temiz-Arpaci O., Kaynak-Onurdag F., Ozgen S.

ZEITSCHRIFT FUR NATURFORSCHUNG SECTION C-A JOURNAL OF BIOSCIENCES, vol.68, pp.453-460, 2013 (SCI-Expanded) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 68
  • Publication Date: 2013
  • Doi Number: 10.5560/znc.2013.68c0453
  • Journal Name: ZEITSCHRIFT FUR NATURFORSCHUNG SECTION C-A JOURNAL OF BIOSCIENCES
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Page Numbers: pp.453-460
  • Keywords: Benzoxazoles, Antibacterial Activity, Antifungal Activity, Antitubercular Activity, ANTIMICROBIAL ACTIVITY, BIOLOGICAL-ACTIVITY
  • Gazi University Affiliated: Yes

Abstract

A new series of 5-(p-substituted benzamido/phenylacetamido)-2-(p-tert-butylphenyl)benzoxazole derivatives were synthesized and evaluated for their antibacterial, antifungal, and antimycobacterial activities against antibiotic-resistant and -sensitive Staphylococcus aureus, Enterococcus faecalis, Escherichia coli, Klebsiella pneumoniae, and Mycobacterium tuberculosis as well as against Candida albicans and Candida krusei. The compounds possessed broad-spectrum activity against all of the tested Gram-positive and Gram-negative bacteria and yeasts, their minimum inhibitory concentrations (MICs) ranging between 16-128 mu g/ml. One compound exhibited significant antibacterial activity (16 mu g/ml) against an antibiotic-resistant Enterococcus faecalis isolate, having twice the potency of the compared standard drugs vancomycin and gentamycin sulfate. The compounds also showed moderate antitubercular activity with MIC values between 8-128 mu g/ml against Mycobacterium tuberculosis and its clinical isolate.