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SYNTHESIS AND ANTIBACTERIAL ACTIVITY OF NOVEL AMIDINO SUBSTITUTED BENZOTHIAZOLES AND BENZIMIDAZOLES

Benzothiazole and benzimidazole scaffolds have become unavoidable structural motifs in the rational drug design because of their versatile pharmacological features. Additionally, it was found that amidines are structural parts of numerous biologically active compounds showing particularly antibacterial and anticancer activity.[1-3] Design of novel amidino derivatives was focused on diversification of three regions of target molecules: changing type of amidino substituent on left-hand side and type substituents on right-hand side of a molecule, as well as changing central heterocycle from benzimidazole to benzothiazole to modulate biological properties. Herein we present the synthesis and in vitro antibacterial activity of novel benzazole amidines. Novel amidino substituted benzazole derivatives were synthesized through formation of benzimidazole moiety by oxidative coupling of o-phenylenediamines with aldehydes or by condensation of 2- aminothiophenoles with corresponding aldehydes to obtain benzothiazole ring. Novel compounds were evaluated for their activity against Gram-positive and Gram-negative bacteria. Pyrimidino-substituted benzimidazoles 14a and 17c showed good antibacterial activity against Gram-positive strain S. pyogenes.

amidino derivatives ; benzimidazole ; benzothiazole ; antibacterial activity

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