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

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

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, vol.39, no.3, pp.291-298, 2004 (SCI-Expanded) identifier identifier identifier


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 mug/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. (C) 2003 Elsevier SAS. All rights reserved.