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The current study was conducted to evaluate the antimicrobial, antioxidant, antileishmanial and cytotoxic potential of designed derivatives of 1,1′-(1,3-phenylenebis(methylene))bis(3-alkyl/aryl-1H-benzimidazol-3-ium) salts. The antibacterial potential of the test compounds was investigated against  Staphylococcus aureus, Pseudomonas aeruginosa  and two methicillin-resistant  S. aureus  (MRSA) strains (MRSA10, MRSA11), where compound  6  showed the best results. For brine shrimp lethality bioassay (BSLB), compound  6  again showed up to 100% mortality at 200 μg/mL and 56.7% mortality at 6.25 μg/mL. Antileishmanial assay was performed against  Leishmania tropica  at 20 μg/mL dosage, where  6  showed the most promising activity with 16.26% survival (83.74% mortality; IC 50 =14.63 μg/mL). The anticancer potential of the selected benzimidazole derivatives was evaluated against two selected cell lines (human colorectal cancer, HCT-116 and breast adenocarcinoma, MCF-7) using sulforhodamine B (SRB) assay. Compound  6  was found to be the most effective cytotoxic compound with 75% inhibition of HCT-116 proliferation at 1 mg/mL concentration. Succinctly,  6  exhibited impressive pharmacological potential that might be attributed to its higher lipophilic character owing to the longer N-substituted alkyl chains when compared to the other test compounds.

Anticancer, antimicrobial and antioxidant potential of sterically tuned bis- N -heterocyclic salts