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Design, and Synthesis of 4-[4-Formyl-3-(2-naphthyl)pyrazol-1-yl]benzoic Acid Derivatives as Potent Growth Inhibitors of Drug-Resistant Staphylococcus aureus.

We report the synthesis and antimicrobial studies of a new series of naphthyl-substituted pyrazole-derived hydrazones. Many of these novel compounds are potent growth inhibitors of several strains of drug-resistant bacteria. These potent compounds have inclined growth inhibitory properties for plank...

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Autores principales: Alnufaie, Rawan, Alsup, Nickolas, Hansa Raj, KC, Newman, Matthew, Whitt, Jedidiah, Chambers, Steven Andrew, Gilmore, David, Alam, Mohammad A.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7655718/
https://www.ncbi.nlm.nih.gov/pubmed/32601342
http://dx.doi.org/10.1038/s41429-020-0341-2
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author Alnufaie, Rawan
Alsup, Nickolas
Hansa Raj, KC
Newman, Matthew
Whitt, Jedidiah
Chambers, Steven Andrew
Gilmore, David
Alam, Mohammad A.
author_facet Alnufaie, Rawan
Alsup, Nickolas
Hansa Raj, KC
Newman, Matthew
Whitt, Jedidiah
Chambers, Steven Andrew
Gilmore, David
Alam, Mohammad A.
author_sort Alnufaie, Rawan
collection PubMed
description We report the synthesis and antimicrobial studies of a new series of naphthyl-substituted pyrazole-derived hydrazones. Many of these novel compounds are potent growth inhibitors of several strains of drug-resistant bacteria. These potent compounds have inclined growth inhibitory properties for planktonic Staphylococcus aureus and Acinetobacter baumannii, and its drug-resistant variants with minimum inhibitory concentration (MIC) as low as 0.78 and 1.56 μg/mL respectively. These compounds also show potent activity against S. aureus and A. baumannii biofilm formation and eradication properties. Time Kill Assay shows that these compounds are bactericidal for S. aureus and bacteriostatic for A. baumannii. The probable mode of action is the disruption of the bacterial cell membrane. Furthermore, potent compounds are nontoxic to human cell lines at several fold higher concentrations than the MICs.
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spelling pubmed-76557182020-12-29 Design, and Synthesis of 4-[4-Formyl-3-(2-naphthyl)pyrazol-1-yl]benzoic Acid Derivatives as Potent Growth Inhibitors of Drug-Resistant Staphylococcus aureus. Alnufaie, Rawan Alsup, Nickolas Hansa Raj, KC Newman, Matthew Whitt, Jedidiah Chambers, Steven Andrew Gilmore, David Alam, Mohammad A. J Antibiot (Tokyo) Article We report the synthesis and antimicrobial studies of a new series of naphthyl-substituted pyrazole-derived hydrazones. Many of these novel compounds are potent growth inhibitors of several strains of drug-resistant bacteria. These potent compounds have inclined growth inhibitory properties for planktonic Staphylococcus aureus and Acinetobacter baumannii, and its drug-resistant variants with minimum inhibitory concentration (MIC) as low as 0.78 and 1.56 μg/mL respectively. These compounds also show potent activity against S. aureus and A. baumannii biofilm formation and eradication properties. Time Kill Assay shows that these compounds are bactericidal for S. aureus and bacteriostatic for A. baumannii. The probable mode of action is the disruption of the bacterial cell membrane. Furthermore, potent compounds are nontoxic to human cell lines at several fold higher concentrations than the MICs. 2020-06-29 2020-12 /pmc/articles/PMC7655718/ /pubmed/32601342 http://dx.doi.org/10.1038/s41429-020-0341-2 Text en Users may view, print, copy, and download text and data-mine the content in such documents, for the purposes of academic research, subject always to the full Conditions of use:http://www.nature.com/authors/editorial_policies/license.html#terms
spellingShingle Article
Alnufaie, Rawan
Alsup, Nickolas
Hansa Raj, KC
Newman, Matthew
Whitt, Jedidiah
Chambers, Steven Andrew
Gilmore, David
Alam, Mohammad A.
Design, and Synthesis of 4-[4-Formyl-3-(2-naphthyl)pyrazol-1-yl]benzoic Acid Derivatives as Potent Growth Inhibitors of Drug-Resistant Staphylococcus aureus.
title Design, and Synthesis of 4-[4-Formyl-3-(2-naphthyl)pyrazol-1-yl]benzoic Acid Derivatives as Potent Growth Inhibitors of Drug-Resistant Staphylococcus aureus.
title_full Design, and Synthesis of 4-[4-Formyl-3-(2-naphthyl)pyrazol-1-yl]benzoic Acid Derivatives as Potent Growth Inhibitors of Drug-Resistant Staphylococcus aureus.
title_fullStr Design, and Synthesis of 4-[4-Formyl-3-(2-naphthyl)pyrazol-1-yl]benzoic Acid Derivatives as Potent Growth Inhibitors of Drug-Resistant Staphylococcus aureus.
title_full_unstemmed Design, and Synthesis of 4-[4-Formyl-3-(2-naphthyl)pyrazol-1-yl]benzoic Acid Derivatives as Potent Growth Inhibitors of Drug-Resistant Staphylococcus aureus.
title_short Design, and Synthesis of 4-[4-Formyl-3-(2-naphthyl)pyrazol-1-yl]benzoic Acid Derivatives as Potent Growth Inhibitors of Drug-Resistant Staphylococcus aureus.
title_sort design, and synthesis of 4-[4-formyl-3-(2-naphthyl)pyrazol-1-yl]benzoic acid derivatives as potent growth inhibitors of drug-resistant staphylococcus aureus.
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7655718/
https://www.ncbi.nlm.nih.gov/pubmed/32601342
http://dx.doi.org/10.1038/s41429-020-0341-2
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