The emergence of multidrug-resistant possesses a significant public health concern. Constitutively expressed MexAB-OprM efflux pumps in significantly contribute to its resistance to a variety of antibiotics. The development of efflux pump inhibitors (EPIs) has emerged as an attractive strategy in reversing antibiotic resistance. In this study, structure-based virtual screening techniques were used for the identification of new MexAB-OprM efflux inhibitors. The predicted poses were thoroughly filtered by induced fit docking procedures followed by microbiological assays for the validation of results. Two compounds, NSC-147850 and NSC-112703, were able to restore tetracycline susceptibility in MexAB-OprM overexpressing ATCC 27853™ strain. This correlation observed between screening and positive efflux inhibitory activity suggests that NSC-147850 and NSC-112703 have potential as EPIs and may be effective in combination therapy against drug-resistant strains of .
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