engleski

Novel symmetric bis-benzimidazoles: Synthesis, DNA/RNA binding and antitrypanosomal activity

The novel benzimidazol-2-yl-fur-5-yl-(1, 2, 3)- triazolyl dimeric series with aliphatic and aromatic central linkers was successfully prepared with the aim of assessing binding affinity to DNA/RNA and antitrypanosomal activity. UV-Visible spectroscopy, thermal denaturation showed interaction of heterocyclic bis-amidines with ctDNA. Circular dichroism studies indicated uniform orientation of heterocyclic bis-amidines along the chiral double helix axis, revealing minor groove binding as the dominant binding mode. The amidino fragment and 1, 4- bis(oxymethylene)phenyl spacer were the main determinants of activity against Trypanosoma brucei. The bis-benzimidazole imidazoline 15c, which had antitrypanosomal potency in the submicromolar range and DNA interacting properties, emerged as a candidate for further structural optimization to obtain more effective agents to combat trypanosome infections.

bis-benzimidazoles ; ctDNA binding ; UV-Vis ; CD spectroscopy ; thermal denaturation ; Trypanosoma brucei

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