Synthesis and antibacterial activity of novel 1,3-diphenyl-1H-pyrazoles functionalized with phenylalanine-derived rhodanines

In the present study, a series of novel 1,3-diphenyl-1H-pyrazoles functionalized with phenylalanine-derived rhodanine derivatives were synthesized and evaluated for their antibacterial activity. Compounds 4, 6, 9, 10, 12 and 15 exhibited stronger activity than the standard drugs, norfloxacin and oxacillin, with MIC values of 1 μg/mL against methicillin-resistant Staphylococcus aureus and quinolone-resistant S. aureus. None of the compounds showed any activity against Gram-negative bacteria.

Fifteen compounds were synthesized and evaluated for their antibacterial activity. Six compounds of 15 tested exhibited stronger activity against MRSA and QRSA with MICs value of 1 μg/mL.Figure optionsDownload as PowerPoint slideHighlights
► A series of 1,3-diphenyl-1H-pyrazoles derivatives were designed and synthesized.
► Most of the synthesized compounds showed significant antibacterial activity.
► Six compounds showed more potent activity against MRSA, QRSA than the standard drugs.