Synthesis and antimicrobial studies of azomethine and N-arylamine derivatives of 4-(4-formyl-3-phenyl-1H-pyrazol-1-yl)benzoic acid as potent anti-methicillin-resistant Staphylococcus aureus agents

Brider, Jamarcus; Rowe, Trent; Gibler, Danielle Jamie; Gottsponer, Adam; Delancey, Evan; Branscum, Michael Drew; Ontko, Allyn C.; Gilmore, David F.; Alam, Mohammad A.

doi:10.1007/s00044-016-1678-8

Cited by 22 publications

(21 citation statements)

References 10 publications

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“…In our efforts to find potent antimicrobial agents [ 13 ], we have previously reported the synthesis of phenyl substituted pyrazole derivatives as potent S. aureus and A. baumannii growth inhibitors [ 14 , 15 ]. Fluoro-substitution on the phenyl ring increased the potency of molecules significantly [ 16 , 17 ].…”

Section: Resultsmentioning

confidence: 99%

Synthesis of 4,4′-(4-Formyl-1H-pyrazole-1,3-diyl)dibenzoic Acid Derivatives as Narrow Spectrum Antibiotics for the Potential Treatment of Acinetobacter Baumannii Infections

Delancey

Allison

et al. 2020

Antibiotics

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Acinetobacter baumannii has emerged as one of the most lethal drug-resistant bacteria in recent years. We report the synthesis and antimicrobial studies of 25 new pyrazole-derived hydrazones. Some of these molecules are potent and specific inhibitors of A. baumannii strains with a minimum inhibitory concentration (MIC) value as low as 0.78 µg/mL. These compounds are non-toxic to mammalian cell lines in in vitro studies. Furthermore, one of the potent molecules has been studied for possible in vivo toxicity in the mouse model and found to be non-toxic based on the effect on 14 physiological blood markers of organ injury.

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Section: Resultsmentioning

confidence: 99%

Synthesis of 4,4′-(4-Formyl-1H-pyrazole-1,3-diyl)dibenzoic Acid Derivatives as Narrow Spectrum Antibiotics for the Potential Treatment of Acinetobacter Baumannii Infections

Delancey

Allison

et al. 2020

Antibiotics

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“…Thiazoline derivative has also been oxidized with DDQ (2,3-dichloro-5,6-dicyanobenzoquinone) to form thiazoles (entry C). 9 In a continuation of our efforts to get novel small molecule heterocycles 10 , 11 by using domino protocol, 12 we report the synthesis of thiazoline and thiazole derivatives using a domino protocol, mild reaction conditions, and readily available substrates ( Scheme 1 ).…”

Section: Resultsmentioning

confidence: 99%

Modular synthesis of thiazoline and thiazole derivatives by using a cascade protocol

Alsharif

Alam

2017

RSC Adv.

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“…13,19 To our delight, we found several molecules with broader and several fold improved activities against both Gram-positive and Gram-negative bacteria. Reaction of 4-hydrazinobenzoic acid ( 1 ) with bisfluoro acetophenyl derivatives ( 2 ) led to the formation of hydrazones ( 3 ).…”

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confidence: 93%

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

Zakeyah

Whitt

Duke

et al. 2018

Bioorganic & Medicinal Chemistry Letters

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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

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Synthesis and antimicrobial studies of azomethine and N-arylamine derivatives of 4-(4-formyl-3-phenyl-1H-pyrazol-1-yl)benzoic acid as potent anti-methicillin-resistant Staphylococcus aureus agents

Cited by 22 publications

References 10 publications

Synthesis of 4,4′-(4-Formyl-1H-pyrazole-1,3-diyl)dibenzoic Acid Derivatives as Narrow Spectrum Antibiotics for the Potential Treatment of Acinetobacter Baumannii Infections

Synthesis of 4,4′-(4-Formyl-1H-pyrazole-1,3-diyl)dibenzoic Acid Derivatives as Narrow Spectrum Antibiotics for the Potential Treatment of Acinetobacter Baumannii Infections

Modular synthesis of thiazoline and thiazole derivatives by using a cascade protocol

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

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