Synthesis and Potent In vitro Activity of Novel 1H‐Benzimidazoles as Anti‐MRSA Agents

A new class of 1H‐benzimidazolecarboxamidines was synthesized and evaluated for in vitro antibacterial and antifungal activities, including drug‐resistant bacterial strains. The most potent compound (32) has the same ratio of anti‐MRSA activity as Vancomycin (minimal inhibitory concentrations value 0.78 μg/mL). The mechanism of action for 1H‐benzimidazolecarboxamidine appears to be different from existing antibacterial agents. These compounds have potential for development as a new class of potent anti‐MRSA agent.

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