Article ID | Journal | Published Year | Pages | File Type |
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1397457 | European Journal of Medicinal Chemistry | 2012 | 5 Pages |
In the present study, a series of 1,3-diaryl pyrazole derivatives bearing rhodanine-3-fatty acid moieties were synthesized and their antimicrobial activities were tested against various Gram-positive and Gram-negative bacteria. 1,3-diaryl-4-formylpyrazoles were synthesized as key intermediates following a Vilsmeier–Haack strategy. Several compounds with an MIC of 2 μg/mL, exhibited stronger antibacterial activity against the methicillin-resistant Staphylococcus aureus (MRSA) than the controls. None of the compounds showed any activity against Gram-negative bacteria.
Graphical abstractA series of 4-functionalized-pyrazoles were synthesized and evaluated for their antibacterial activity.Figure optionsDownload full-size imageDownload as PowerPoint slideHighlights► We introduced different substitutes at N-3 and C-5 position of rhodanine. ► Most of the compounds showed good antibacterial activity even at low concentration. ► Several compounds were more potent than the controls against MRSA.