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Low-Molecular Pyrazine-Based DNA Binders: Physicochemical and Antimicrobial Properties

Pyrazine and its derivatives are a large group of compounds that exhibit broad biological activity, the changes of which can be easily detected by a substituent effect or a change in the functional group. The present studies combined theoretical research with the density functional theory (DFT) appr...

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Autores principales: Mech-Warda, Paulina, Giełdoń, Artur, Kawiak, Anna, Maciejewska, Natalia, Olszewski, Mateusz, Makowski, Mariusz, Chylewska, Agnieszka
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2022
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9228100/
https://www.ncbi.nlm.nih.gov/pubmed/35744829
http://dx.doi.org/10.3390/molecules27123704
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author Mech-Warda, Paulina
Giełdoń, Artur
Kawiak, Anna
Maciejewska, Natalia
Olszewski, Mateusz
Makowski, Mariusz
Chylewska, Agnieszka
author_facet Mech-Warda, Paulina
Giełdoń, Artur
Kawiak, Anna
Maciejewska, Natalia
Olszewski, Mateusz
Makowski, Mariusz
Chylewska, Agnieszka
author_sort Mech-Warda, Paulina
collection PubMed
description Pyrazine and its derivatives are a large group of compounds that exhibit broad biological activity, the changes of which can be easily detected by a substituent effect or a change in the functional group. The present studies combined theoretical research with the density functional theory (DFT) approach (B3LYP/6-311+G**) and experimental (potentiometric and spectrophotometric) analysis for a thorough understanding of the structure of chlorohydrazinopyrazine, its physicochemical and cytotoxic properties, and the site and nature of interaction with DNA. The obtained results indicated that 2-chloro-3-hydrazinopyrazine (2Cl3HP) displayed the highest affinity to DNA. Cytotoxicity studies revealed that the compound did not exhibit toxicity toward human dermal keratinocytes, which supported the potential application of 2Cl3HP in clinical use. The study also attempted to establish the possible equilibria occurring in the aqueous solution and, using both theoretical and experimental methods, clearly showed the hydrophilic nature of the compound. The experimental and theoretical results of the study confirmed the quality of the compound, as well as the appropriateness of the selected set of methods for similar research.
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spelling pubmed-92281002022-06-25 Low-Molecular Pyrazine-Based DNA Binders: Physicochemical and Antimicrobial Properties Mech-Warda, Paulina Giełdoń, Artur Kawiak, Anna Maciejewska, Natalia Olszewski, Mateusz Makowski, Mariusz Chylewska, Agnieszka Molecules Article Pyrazine and its derivatives are a large group of compounds that exhibit broad biological activity, the changes of which can be easily detected by a substituent effect or a change in the functional group. The present studies combined theoretical research with the density functional theory (DFT) approach (B3LYP/6-311+G**) and experimental (potentiometric and spectrophotometric) analysis for a thorough understanding of the structure of chlorohydrazinopyrazine, its physicochemical and cytotoxic properties, and the site and nature of interaction with DNA. The obtained results indicated that 2-chloro-3-hydrazinopyrazine (2Cl3HP) displayed the highest affinity to DNA. Cytotoxicity studies revealed that the compound did not exhibit toxicity toward human dermal keratinocytes, which supported the potential application of 2Cl3HP in clinical use. The study also attempted to establish the possible equilibria occurring in the aqueous solution and, using both theoretical and experimental methods, clearly showed the hydrophilic nature of the compound. The experimental and theoretical results of the study confirmed the quality of the compound, as well as the appropriateness of the selected set of methods for similar research. MDPI 2022-06-09 /pmc/articles/PMC9228100/ /pubmed/35744829 http://dx.doi.org/10.3390/molecules27123704 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
Mech-Warda, Paulina
Giełdoń, Artur
Kawiak, Anna
Maciejewska, Natalia
Olszewski, Mateusz
Makowski, Mariusz
Chylewska, Agnieszka
Low-Molecular Pyrazine-Based DNA Binders: Physicochemical and Antimicrobial Properties
title Low-Molecular Pyrazine-Based DNA Binders: Physicochemical and Antimicrobial Properties
title_full Low-Molecular Pyrazine-Based DNA Binders: Physicochemical and Antimicrobial Properties
title_fullStr Low-Molecular Pyrazine-Based DNA Binders: Physicochemical and Antimicrobial Properties
title_full_unstemmed Low-Molecular Pyrazine-Based DNA Binders: Physicochemical and Antimicrobial Properties
title_short Low-Molecular Pyrazine-Based DNA Binders: Physicochemical and Antimicrobial Properties
title_sort low-molecular pyrazine-based dna binders: physicochemical and antimicrobial properties
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9228100/
https://www.ncbi.nlm.nih.gov/pubmed/35744829
http://dx.doi.org/10.3390/molecules27123704
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