A series of 2-arylindoles were synthesized and characterized through spectral analysis. Their antibacterial activity and synergistic effect against multidrug-resistant Staphylococcus aureus were pharmacologically studied. 2-(4-Aminophenyl)-1H-indole (4k) showed a potent inhibitory activity at 15.6 μg/ml against Bacillus subtilis ATCC 6633 and Salmonella typhi ATCC 19430. 2-(3-Nitrophenyl)-1H-indole (4j) at 15.6 μg/ml displayed a potent antibacterial activity only against S. typhi ATCC 19430. All the synthesized compounds elicited a synergistic effect against methicillin-resistant S. aureus Sp6, drug resistance, and efflux pump genes strain. 2-(2-Hydroxyphenyl)-1Hindoles 4g, 4j, and 4k were combined with tetracyclines, thereby decreasing the minimum inhibitory concentration of tetracyclines. Molecular docking showed that interaction with key amino acids occurred at the active site of the NorA efflux pump. Prediction of the toxicity using the ADMET study was also reported.
Key words: 2-arylindoles, antibacterial activity, synergistic effects, MRSA efflux inhibitor
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