Synthesis and biological activity of amidino substituted benzimidazoles and benzothiazoles

Due to the great biological importance of benzimidazole and benzothiazole derived derivatives, nowadays there is still an increasing interest in medicinal and pharmaceutical chemistry for using this unavoidable structural motifs in the rational design of novel drugs. Suchlike derivatives display a broad spectrum of different biological features such as anticancer, antiviral, antioxidant, antibacterial, antifungal, antihistaminic, anti-inflammatory, etc. Amidines are structural parts of numerous biologically active compounds like many important medical and biochemical agents. By introduction of amidino functional groups at the termini of the molecule, the biological activity could be significantly improved because of interaction with an electronegatively charged biological molecule such as DNA. Herein we present the synthesis and biological evaluation of novel amidino substituted benzimidazole and benzothiazole derivatives substituted with 2-hydroxyphehyl ring in the position 2. All compounds were tested for their antiproliferative activity on several human cancer cells as well as for antibacterial activity in vitro.