Small molecule based inhibitors development is a growing field in medicinal chemistry. In recent years, different heterocyclic derivatives have been designed to counter the infections caused by multi-drug resistant bacteria. Indeed, small molecule inhibitors can be employed as an efficient antibacterial agents with different mechanism of action. Methicillin-resistant Staphylococcus aureus (MRSA) is becoming lethal to mankind due to easy transmission mode, rapid resistance development to existing antibiotics and affect difficult-to-treat skin and filmsy diseases. Benzimidazoles are a class of heterocyclic compounds which have capability to fight against MRSA. High biocompatibility of benzimidazoles, synergistic behaviour with antibiotics and their tunable physico-chemical properties attracted the researchers to develop new benzimidazole based antibacterial agents. The present review focus on recent developments of benzimidazole-hybrid molecules as anti MRSA agents and the results of in-vitro and in-vivo studies with possible mechanism of action and discussing structure-activity relationship (SAR) in different directions. Benzimdazoles act as DNA binding agents, enzyme inhibitors, anti-biofilm agents and showed synergistic effect with available antibiotics to achieve antibacterial activity against MRSA. This cumulative figures would help to design new benzimidazole-based MRSA growth inhibitors.
Keywords: Antibiotics; Benzimidazole; DNA binding agents; Drug resistance; MRSA.
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