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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

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...

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Detalles Bibliográficos
Autores principales: Delancey, Evan, Allison, Devin, KC, Hansa Raj, Gilmore, David F., Fite, Todd, Basnakian, Alexei G., Alam, Mohammad A.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7601628/
https://www.ncbi.nlm.nih.gov/pubmed/32998384
http://dx.doi.org/10.3390/antibiotics9100650
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author Delancey, Evan
Allison, Devin
KC, Hansa Raj
Gilmore, David F.
Fite, Todd
Basnakian, Alexei G.
Alam, Mohammad A.
author_facet Delancey, Evan
Allison, Devin
KC, Hansa Raj
Gilmore, David F.
Fite, Todd
Basnakian, Alexei G.
Alam, Mohammad A.
author_sort Delancey, Evan
collection PubMed
description 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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spelling pubmed-76016282020-11-01 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, Evan Allison, Devin KC, Hansa Raj Gilmore, David F. Fite, Todd Basnakian, Alexei G. Alam, Mohammad A. Antibiotics (Basel) Article 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. MDPI 2020-09-28 /pmc/articles/PMC7601628/ /pubmed/32998384 http://dx.doi.org/10.3390/antibiotics9100650 Text en © 2020 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
Delancey, Evan
Allison, Devin
KC, Hansa Raj
Gilmore, David F.
Fite, Todd
Basnakian, Alexei G.
Alam, Mohammad A.
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
title 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
title_full 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
title_fullStr 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
title_full_unstemmed 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
title_short 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
title_sort 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
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7601628/
https://www.ncbi.nlm.nih.gov/pubmed/32998384
http://dx.doi.org/10.3390/antibiotics9100650
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