Pyridine Derivatives—A New Class of Compounds That Are Toxic to E. coli K12, R2–R4 Strains
| Autor: | Paweł Śmigielski, Karol Kramkowski, Mateusz Szymczak, Paweł Kowalczyk, Ryszard Ostaszewski, Jacek A. Michalski, Kamil Gawin, Magdalena Laskowska, Rafał Lizut, Anastasiia Hrunyk, Łukasz Laskowski, Dominik Koszelewski |
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| Jazyk: | angličtina |
| Rok vydání: | 2021 |
| Předmět: |
Technology
Lipopolysaccharide medicine.drug_class E. coli strains Antibiotics medicine.disease_cause Article antibiotics chemistry.chemical_compound medicine oxidative stress General Materials Science Escherichia coli Malononitrile Microscopy QC120-168.85 biology Chemistry QH201-278.5 lipopolysaccharide Biological activity Engineering (General). Civil engineering (General) Antimicrobial biology.organism_classification TK1-9971 pyridine derivatives Descriptive and experimental mechanics Biochemistry Electrical engineering. Electronics. Nuclear engineering TA1-2040 Antibacterial activity Bacteria |
| Zdroj: | Materials Volume 14 Issue 18 Materials, Vol 14, Iss 5401, p 5401 (2021) |
| ISSN: | 1996-1944 |
| Popis: | A preliminary study of 2-amino-4-aryl-3,5-dicarbonitrile-6-thiopyridines as new potential antimicrobial drugs was performed. Special emphasis was placed on the selection of the structure of target pyridine derivatives with the highest biological activity against different types of Gram-stained bacteria by lipopolysaccharide (LPS). Herein, Escherichia coli model strains K12 (without LPS in its structure) and R2–R4 (with different lengths of LPS in its structure) were used. Studied target compounds were provided with yields ranging from 53% to 91% by the lipase-catalyzed one pot multicomponent reaction of various aromatic aldehydes with malononitrile, and thiols. The presented work showed that the antibacterial activity of the studied pyridines depends on their structure and affects the LPS of bacteria. Moreover, the influence of the pyridines on bacteria possessing smooth and rough LPS and oxidative damage to plasmid DNA caused by investigated compounds was indicated. Additionally, the modification of the bacterial DNA with the tested compounds was performed to detect new potential oxidative damages, which are recognized by the Fpg protein. The obtained damage modification values of the analyzed compounds were compared with the modifications after antibiotics were used in this type of research. The presented studies demonstrate that 2-amino-4-aryl-3,5-dicarbonitrile-6-thiopyridines can be used as substitutes for known antibiotics. The observed results are especially important in the case of the increasing resistance of bacteria to various drugs and antibiotics. |
| Databáze: | OpenAIRE |
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