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Background  The emergence of bacterial resistance is a major public health problem. It is essential to develop and synthesize new therapeutic agents with better activity. The mode of actions of certain newly developed antimicrobial agents, however, exhibited very limited effect in treating life threatening systemic infections. Therefore, the advancement of multi-potent and efficient antimicrobial agents is crucial to overcome the increased multi-drug resistance of bacteria and fungi. Cancer, which remains as one of the primary causes of deaths and is commonly treated by chemotherapeutic agents, is also in need of novel and efficacious agents to treat resistant cases. As such, a sequence of novel substituted benzamides was designed, synthesized and evaluated for their antimicrobial and anticancer activities.    Methodology  All synthesized compounds were characterized by IR, NMR, Mass and elemental analysis followed by in vitro antimicrobial studies against Gram-positive ( Staphylococcus aureus ), Gram-negative ( Salmonella typhi  and  Klebsiella pneumoniae ) bacterial and fungal ( Candida albicans  and  Aspergillus niger ) strains by the tube dilution method. The in vitro anticancer evaluation was carried out against the human colorectal carcinoma cell line (HCT116), using the Sulforhodamine B assay.    Results, discussion and conclusion  Compound  W6  (MIC  sa, st, kp   = 5.19 µM) emerged as a significant antibacterial agent against all tested bacterial strains  i.e.  Gram-positive ( S. aureus ), Gram-negative ( S. typhi, K. pneumoniae ) while compound  W1  (MIC  ca, an   = 5.08 µM) was most potent against fungal strains ( A. niger  and  C. albicans ) and comparable to fluconazole (MIC = 8.16 µM). The anticancer screening demonstrated that compound  W17  (IC 50  = 4.12 µM) was most potent amongst the synthesized  compounds and also more potent than the standard drug 5-FU (IC 50  = 7.69 µM).

Design, synthesis and therapeutic potential of 3-(2-(1H-benzo[d]imidazol-2-ylthio)acetamido)-N-(substituted phenyl)benzamide analogues