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

Eur J Med Chem

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ankara University, Tandogan, 06100 Ankara, Turkey.

Published: March 2004

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 microg/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.

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http://dx.doi.org/10.1016/j.ejmech.2003.11.014DOI Listing

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