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The Evaluation of DHPMs as Biotoxic Agents on Pathogen Bacterial Membranes

Herein, we present biological studies on 3,4-dihydropyrimidin-2(1H)-ones (DHPMs) obtained via Biginelli reaction catalyzed by NH4Cl under solvent-free conditions. Until now, DHPMs have not been tested for biological activity against pathogenic E. coli strains. We tested 16 newly synthesized DHPMs as...

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Autores principales: Gawdzik, Barbara, Kowalczyk, Paweł, Koszelewski, Dominik, Brodzka, Anna, Masternak, Joanna, Kramkowski, Karol, Wypych, Aleksandra, Ostaszewski, Ryszard
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2022
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8878598/
https://www.ncbi.nlm.nih.gov/pubmed/35207159
http://dx.doi.org/10.3390/membranes12020238
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author Gawdzik, Barbara
Kowalczyk, Paweł
Koszelewski, Dominik
Brodzka, Anna
Masternak, Joanna
Kramkowski, Karol
Wypych, Aleksandra
Ostaszewski, Ryszard
author_facet Gawdzik, Barbara
Kowalczyk, Paweł
Koszelewski, Dominik
Brodzka, Anna
Masternak, Joanna
Kramkowski, Karol
Wypych, Aleksandra
Ostaszewski, Ryszard
author_sort Gawdzik, Barbara
collection PubMed
description Herein, we present biological studies on 3,4-dihydropyrimidin-2(1H)-ones (DHPMs) obtained via Biginelli reaction catalyzed by NH4Cl under solvent-free conditions. Until now, DHPMs have not been tested for biological activity against pathogenic E. coli strains. We tested 16 newly synthesized DHPMs as antimicrobial agents on model E. coli strains (K12 and R2–R4). Preliminary cellular studies using MIC and MBC tests and digestion of Fpg after modification of bacterial DNA suggest that these compounds may have greater potential as antibacterial agents than typically used antibiotics, such as ciprofloxacin (ci), bleomycin (b) and cloxacillin (cl). The described compounds are highly specific for pathogenic E. coli strains based on the model strains used and may be engaged in the future as new substitutes for commonly used antibiotics in clinical and nosocomial infections in the pandemic era.
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spelling pubmed-88785982022-02-26 The Evaluation of DHPMs as Biotoxic Agents on Pathogen Bacterial Membranes Gawdzik, Barbara Kowalczyk, Paweł Koszelewski, Dominik Brodzka, Anna Masternak, Joanna Kramkowski, Karol Wypych, Aleksandra Ostaszewski, Ryszard Membranes (Basel) Article Herein, we present biological studies on 3,4-dihydropyrimidin-2(1H)-ones (DHPMs) obtained via Biginelli reaction catalyzed by NH4Cl under solvent-free conditions. Until now, DHPMs have not been tested for biological activity against pathogenic E. coli strains. We tested 16 newly synthesized DHPMs as antimicrobial agents on model E. coli strains (K12 and R2–R4). Preliminary cellular studies using MIC and MBC tests and digestion of Fpg after modification of bacterial DNA suggest that these compounds may have greater potential as antibacterial agents than typically used antibiotics, such as ciprofloxacin (ci), bleomycin (b) and cloxacillin (cl). The described compounds are highly specific for pathogenic E. coli strains based on the model strains used and may be engaged in the future as new substitutes for commonly used antibiotics in clinical and nosocomial infections in the pandemic era. MDPI 2022-02-18 /pmc/articles/PMC8878598/ /pubmed/35207159 http://dx.doi.org/10.3390/membranes12020238 Text en © 2022 by the authors. https://creativecommons.org/licenses/by/4.0/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 (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Gawdzik, Barbara
Kowalczyk, Paweł
Koszelewski, Dominik
Brodzka, Anna
Masternak, Joanna
Kramkowski, Karol
Wypych, Aleksandra
Ostaszewski, Ryszard
The Evaluation of DHPMs as Biotoxic Agents on Pathogen Bacterial Membranes
title The Evaluation of DHPMs as Biotoxic Agents on Pathogen Bacterial Membranes
title_full The Evaluation of DHPMs as Biotoxic Agents on Pathogen Bacterial Membranes
title_fullStr The Evaluation of DHPMs as Biotoxic Agents on Pathogen Bacterial Membranes
title_full_unstemmed The Evaluation of DHPMs as Biotoxic Agents on Pathogen Bacterial Membranes
title_short The Evaluation of DHPMs as Biotoxic Agents on Pathogen Bacterial Membranes
title_sort evaluation of dhpms as biotoxic agents on pathogen bacterial membranes
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8878598/
https://www.ncbi.nlm.nih.gov/pubmed/35207159
http://dx.doi.org/10.3390/membranes12020238
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