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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...
Autores principales: | , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
2020
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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. |
format | Online Article Text |
id | pubmed-7655718 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2020 |
record_format | MEDLINE/PubMed |
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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