Taking into account that benzimidazole, benzothiazole and benzoxazole nuclei, as a part of nitrogen
heterocycles, are highly-privileged building structural motifs in organic and medicinal chemistry, they
played unavoidable role in the rational drug design. Among their versatile pharmacological features, the
most important ones are antimicrobial, antitumor, antiviral, anti-inflammanory, antihistaminic,
antioxidant, etc. On the other hand, amidines are known as important pharmacophore functional groups
usually placed at the termini of the biologically active molecules. They are a structural parts of the
numerous biologically active compounds and many important medical and biochemical agents. Amidine
groups, usually in cationic form, could significantly contribute to the molecule/possible biological target
complex stability. Herein we present the synthesis, structural characterization and biological evaluation
of amidino substituted benzimidazole and benzothiazole derivatives substituted with 2-naphthyl ring. All
targeted compounds have been synthesized according to the conventional methods of organic synthesis.
They have been evaluated on the several human cancer cell lines for their antiproliferative activity in vitro.
Additionally, all synthesized compounds have been tested against several Gram negative and Gram
positive bacterial strains in vitro.
