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1.
Molecules ; 29(16)2024 Aug 11.
Article in English | MEDLINE | ID: mdl-39202893

ABSTRACT

Nowadays, searching for novel antimicrobial agents is crucial due to the increasing number of resistant bacterial strains. Moreover, cancer therapy is a major challenge for modern medicine. Currently used cytostatics have a large number of side effects and insufficient therapeutic effects. Due to the above-mentioned facts, we undertook research to synthesize novel compounds from the acylhydrazone group aimed at obtaining potential antimicrobial and anticancer agents. As a starting material, we employed hydrazides of 2-, 3- or 4-iodobenzoic acid, which gave three series of acylhydrazones in the condensation reaction with various aldehydes. The chemical structure of all obtained compounds was confirmed by IR, 1H NMR, and 13C NMR. The structure of selected compounds was determined by single-crystal X-ray diffraction analysis. Additionally, all samples were characterized using powder X-ray diffraction. The other issue in this research was to examine the possibility of the solvent-free synthesis of compounds using mechanochemical methods. The biological screening results revealed that some of the newly synthesized compounds indicated a beneficial antimicrobial effect even against MRSA-the methicillin-resistant Staphylococcus aureus ATCC 43300 strain. In many cases, the antibacterial activity of synthesized acylhydrazones was equal to or better than that of commercially available antibacterial agents that were used as reference substances in this research. Significantly, the tested compounds do not show toxicity to normal cell lines either.


Subject(s)
Anti-Bacterial Agents , Hydrazones , Microbial Sensitivity Tests , Hydrazones/chemistry , Hydrazones/pharmacology , Hydrazones/chemical synthesis , Humans , Anti-Bacterial Agents/pharmacology , Anti-Bacterial Agents/chemistry , Anti-Bacterial Agents/chemical synthesis , Iodobenzoates/chemistry , Antineoplastic Agents/pharmacology , Antineoplastic Agents/chemistry , Antineoplastic Agents/chemical synthesis , Molecular Structure , Methicillin-Resistant Staphylococcus aureus/drug effects , Crystallography, X-Ray , Structure-Activity Relationship , Anti-Infective Agents/pharmacology , Anti-Infective Agents/chemistry , Anti-Infective Agents/chemical synthesis
2.
Chem Biol Drug Des ; 104(1): e14590, 2024 Jul.
Article in English | MEDLINE | ID: mdl-39039615

ABSTRACT

Hydrazones display an interesting profile of biological activities, which includes mainly antimicrobial and antiproliferative properties. Hydrazones also play an important role in the synthesis of heterocyclic rings and in coordination chemistry. Currently, the synthesis of complexes of hydrazones with transition metals is quite frequently reported in the scientific literature. The interest in this topic is largely due to diverse biological activities of the metal complexes of hydrazones that in some cases are much more effective than hydrazones themselves. This review focuses on the complexes of hydrazones with transition metals which display antibacterial, antitubercular, antifungal and anticancer activities. In the following subchapters devoted to a given activity, an attempt has been made to present the most active complexes of hydrazones, their trends in their activity and application in medicinal chemistry. The paper presents the literature data from 2009 to 2023. This review constitutes a useful guide for the researchers who intend to synthesize and investigate complexes of hydrazones in terms of their antimicrobial and anticancer activities.


Subject(s)
Anti-Infective Agents , Antineoplastic Agents , Coordination Complexes , Hydrazones , Transition Elements , Hydrazones/chemistry , Hydrazones/pharmacology , Hydrazones/chemical synthesis , Antineoplastic Agents/chemistry , Antineoplastic Agents/pharmacology , Antineoplastic Agents/chemical synthesis , Transition Elements/chemistry , Transition Elements/pharmacology , Coordination Complexes/chemistry , Coordination Complexes/pharmacology , Coordination Complexes/chemical synthesis , Humans , Anti-Infective Agents/pharmacology , Anti-Infective Agents/chemistry , Anti-Infective Agents/chemical synthesis , Neoplasms/drug therapy
3.
Med Dosw Mikrobiol ; 55(3): 219-24, 2003.
Article in Polish | MEDLINE | ID: mdl-14702663

ABSTRACT

The purpose of the study was to characterize fermentation of sucrose by Escherichia coli strains and to answer why some of these strains doesn't utilize this disaccharide. Investigations included 16 E. coli strains. Only 5 of these strains utilized sucrose. Genotypic analysis demonstrated the presence of cscB gene (encoding the sucrase permease which catalyzes transport of sucrose through the plasma membrane of the cell) in 5 strains of E. coli and cscA gene (encoding an enzyme sucrase that catalyzes the utilization of sucrose) in 6 strains of E. coli. These 5 of E. coli strains which possessed a chromosomally encoded sucrose metabolic pathway utilized sucrose with a different time. 3 of them destroyed this disaccharide after 24 h and 2 of them destroyed it after 48 h. Ten of E. coli strains hadn't cscA gene and 11 of them had not cscB genes. The lack of these genes can be the prove that it is not possible for 11 of E. coli strains to synthesize sucrose permease and for 10 of them to synthesize sucrase and it may be the reason of not utilize disaccharide sucrose by these bacteria.


Subject(s)
Escherichia coli/enzymology , Escherichia coli/genetics , Sucrose/metabolism , Fermentation , Genotype , Membrane Transport Proteins/genetics , Phenotype , Sucrase/genetics
4.
Przegl Epidemiol ; 57(2): 263-70, 2003.
Article in Polish | MEDLINE | ID: mdl-12910593

ABSTRACT

The purpose of the work has been to identify Yersinia pseudotuberculosis strains and to demonstrate their potential pathogenicity using PCR reaction. Investigations included 167 samples of the water and 32 samples of the soil from westpomeranian region. Based on the analysis of PCR reactions the research confirmed the presence of DNA Y. pseudotuberculosis strain in 6 of the water samples and in 1 of the soil sample. The strains have been identified by nucleotide sequence of the ypm gene, which is specific only for mentioned species. Genotypic analysis demonstrated also the presence of genes, which confirmed their virulence. The PCR reaction should be used in the microbiological diagnostic of Y. pseudotuberculosis strains, isolated from animals and from environment, because it is very specific, fast and sensitive method.


Subject(s)
Disease Outbreaks/prevention & control , Environment , Yersinia pseudotuberculosis Infections/epidemiology , Yersinia pseudotuberculosis Infections/microbiology , Yersinia pseudotuberculosis/isolation & purification , Bacterial Proteins/genetics , DNA, Viral/genetics , Humans , Polymerase Chain Reaction , Soil Microbiology , Water Microbiology , Yersinia pseudotuberculosis/genetics , Yersinia pseudotuberculosis Infections/genetics
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