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. 2018 Sep 15;28(17):2914-2919.
doi: 10.1016/j.bmcl.2018.07.016. Epub 2018 Jul 10.

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

A A Zakeyah  1 , J Whitt  1 , C Duke  1 , D F Gilmore  2 , D G Meeker  3 , M S Smeltzer  3 , M A Alam  4
Affiliations

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

A A Zakeyah et al. Bioorg Med Chem Lett. .

Abstract

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.

Keywords: Acinetobacter baumannii; Antimicrobial; Hydrazone; MRSA; Pyrazole.

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Figures

Fig. 1.
Fig. 1.
Pyrazole derived hydrazones as potent antimicrobial agents.
Fig. 2.
Fig. 2.
Cytotoxic assay of active compounds on HEK293 cell line by using resazurin assay.
Scheme 1.
Scheme 1.
Synthesis of bisfluorophenyl pyrazole-derived aldehyde.
See this image and copyright information in PMC

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