Synthesis and antimicrobial studies of hydrazone derivatives of 4-[3-(2,4-difluorophenyl)-4-formyl-1H-pyrazol-1-yl]benzoic acid and 4-[3-(3,4-difluorophenyl)-4-formyl-1H-pyrazol-1-yl]benzoic acid

[Display omitted] •Benign synthesis of new pyrazole derivatives.•29 novel molecules.•MIC as low as 0.78 μM (S. aureus, MRSA, B. subtilis, and A. baumannii).•Non-toxic to mammalian cells.•Potential LpxM inhibitors. Microbial resistance to antibiotics is an unresolved global concern, which needs urgen...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2018-09, Vol.28 (17), p.2914-2919
Hauptverfasser: Zakeyah, A.A., Whitt, J., Duke, C., Gilmore, D.F., Meeker, D.G., Smeltzer, M.S., Alam, M.A.
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Sprache:eng
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Zusammenfassung:[Display omitted] •Benign synthesis of new pyrazole derivatives.•29 novel molecules.•MIC as low as 0.78 μM (S. aureus, MRSA, B. subtilis, and A. baumannii).•Non-toxic to mammalian cells.•Potential LpxM inhibitors. Microbial resistance to antibiotics is an unresolved global concern, which needs urgent and coordinated action. One of the guidelines of the Centers for Disease Control and Preventions (CDC) to combat antibiotic resistance is the development of new antibiotics to treat drug-resistant bacteria. In our effort to find new antibiotics, we report the synthesis and antimicrobial studies of 30 new pyrazole derivatives. These novel molecules have been synthesized by using readily available starting materials and benign reaction conditions. Some of these molecules have shown activity with MIC values as low as 0.78 µg/mL against four bacterial strains; Staphylococcus aureus, methicillin-resistant S. aureus, Bacillus subtilis, and Acinetobacter baumannii. Furthermore, active molecules are non-toxic to mammalian cell line.▪
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2018.07.016