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Synthesis of Hydrazone Derivatives of 4-[4-Formyl-3-(2-oxochromen-3-yl)pyrazol-1-yl]benzoic acid as Potent Growth Inhibitors of Antibiotic-resistant Staphylococcus aureus and Acinetobacter baumannii

Microbial resistance to drugs is an unresolved global concern, which is present in every country. Developing new antibiotics is one of the guidelines of the Centers for Disease Control and Preventions (CDC) to combat bacterial resistance to drugs. Based on our lead molecules, we report the synthesis...

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Autores principales: Whitt, Jedidiah, Duke, Cameron, Sumlin, Anthony, Chambers, Steven A., Alnufaie, Rawan, Gilmore, David, Fite, Todd, Basnakian, Alexei G., Alam, Mohammad A.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2019
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6600224/
https://www.ncbi.nlm.nih.gov/pubmed/31146470
http://dx.doi.org/10.3390/molecules24112051
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author Whitt, Jedidiah
Duke, Cameron
Sumlin, Anthony
Chambers, Steven A.
Alnufaie, Rawan
Gilmore, David
Fite, Todd
Basnakian, Alexei G.
Alam, Mohammad A.
author_facet Whitt, Jedidiah
Duke, Cameron
Sumlin, Anthony
Chambers, Steven A.
Alnufaie, Rawan
Gilmore, David
Fite, Todd
Basnakian, Alexei G.
Alam, Mohammad A.
author_sort Whitt, Jedidiah
collection PubMed
description Microbial resistance to drugs is an unresolved global concern, which is present in every country. Developing new antibiotics is one of the guidelines of the Centers for Disease Control and Preventions (CDC) to combat bacterial resistance to drugs. Based on our lead molecules, we report the synthesis and antimicrobial studies of 27 new pyrazole derivatives. These new coumarin-pyrazole-hydrazone hybrids are readily synthesized from commercially available starting materials and reagents using benign reaction conditions. All the synthesized molecules were tested against 14 Gram-positive and Gram-negative bacterial strains. Several of these molecules have been found to be potent growth inhibitors of several strains of these tested bacteria with minimum inhibitory concentrations as low as 1.56 μg/mL. Furthermore, active molecules are non-toxic in in vitro and in vivo toxicity studies.
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spelling pubmed-66002242019-07-16 Synthesis of Hydrazone Derivatives of 4-[4-Formyl-3-(2-oxochromen-3-yl)pyrazol-1-yl]benzoic acid as Potent Growth Inhibitors of Antibiotic-resistant Staphylococcus aureus and Acinetobacter baumannii Whitt, Jedidiah Duke, Cameron Sumlin, Anthony Chambers, Steven A. Alnufaie, Rawan Gilmore, David Fite, Todd Basnakian, Alexei G. Alam, Mohammad A. Molecules Article Microbial resistance to drugs is an unresolved global concern, which is present in every country. Developing new antibiotics is one of the guidelines of the Centers for Disease Control and Preventions (CDC) to combat bacterial resistance to drugs. Based on our lead molecules, we report the synthesis and antimicrobial studies of 27 new pyrazole derivatives. These new coumarin-pyrazole-hydrazone hybrids are readily synthesized from commercially available starting materials and reagents using benign reaction conditions. All the synthesized molecules were tested against 14 Gram-positive and Gram-negative bacterial strains. Several of these molecules have been found to be potent growth inhibitors of several strains of these tested bacteria with minimum inhibitory concentrations as low as 1.56 μg/mL. Furthermore, active molecules are non-toxic in in vitro and in vivo toxicity studies. MDPI 2019-05-29 /pmc/articles/PMC6600224/ /pubmed/31146470 http://dx.doi.org/10.3390/molecules24112051 Text en © 2019 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Whitt, Jedidiah
Duke, Cameron
Sumlin, Anthony
Chambers, Steven A.
Alnufaie, Rawan
Gilmore, David
Fite, Todd
Basnakian, Alexei G.
Alam, Mohammad A.
Synthesis of Hydrazone Derivatives of 4-[4-Formyl-3-(2-oxochromen-3-yl)pyrazol-1-yl]benzoic acid as Potent Growth Inhibitors of Antibiotic-resistant Staphylococcus aureus and Acinetobacter baumannii
title Synthesis of Hydrazone Derivatives of 4-[4-Formyl-3-(2-oxochromen-3-yl)pyrazol-1-yl]benzoic acid as Potent Growth Inhibitors of Antibiotic-resistant Staphylococcus aureus and Acinetobacter baumannii
title_full Synthesis of Hydrazone Derivatives of 4-[4-Formyl-3-(2-oxochromen-3-yl)pyrazol-1-yl]benzoic acid as Potent Growth Inhibitors of Antibiotic-resistant Staphylococcus aureus and Acinetobacter baumannii
title_fullStr Synthesis of Hydrazone Derivatives of 4-[4-Formyl-3-(2-oxochromen-3-yl)pyrazol-1-yl]benzoic acid as Potent Growth Inhibitors of Antibiotic-resistant Staphylococcus aureus and Acinetobacter baumannii
title_full_unstemmed Synthesis of Hydrazone Derivatives of 4-[4-Formyl-3-(2-oxochromen-3-yl)pyrazol-1-yl]benzoic acid as Potent Growth Inhibitors of Antibiotic-resistant Staphylococcus aureus and Acinetobacter baumannii
title_short Synthesis of Hydrazone Derivatives of 4-[4-Formyl-3-(2-oxochromen-3-yl)pyrazol-1-yl]benzoic acid as Potent Growth Inhibitors of Antibiotic-resistant Staphylococcus aureus and Acinetobacter baumannii
title_sort synthesis of hydrazone derivatives of 4-[4-formyl-3-(2-oxochromen-3-yl)pyrazol-1-yl]benzoic acid as potent growth inhibitors of antibiotic-resistant staphylococcus aureus and acinetobacter baumannii
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6600224/
https://www.ncbi.nlm.nih.gov/pubmed/31146470
http://dx.doi.org/10.3390/molecules24112051
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