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Spectral, thermal, antimicrobial studies for silver(I) complexes of pyrazolone derivatives.

ABSTRACT: Background: Synthesize new complexes of Ag(I) to enhance efficacy or stability and also, pharmacological activities on the operation of pyrazolone's biological properties.

Results: Efficient and high yielding pathways starting from the versatile and readily available 3-methyl-1-phenyl-5-pyrazolone by Knoevenagel condensation of a sequence of 4-arylidene-3-methyl-1-phenyl-5-pyrazolone derivatives (2a-c) have been formed by the reaction of various substituted aromatic aldehydes Used as ligands to synthesize Ag(I) chelates. Synthesized compounds and their complexes have been characterized by elemental analysis, magnetic and spectroscopic methods (IR, ¹³C, ¹HNMR, mass) and thermal analysis. The spectrophotometric determinations suggest distorted octaedral geometry for all complexes. Both ligands and their metal complexes have also been tested for their antibacterial and antifungal efficacy.

Conclusions: Newly synthesized compounds have shown potent antimicrobial activity. The results showed that the complex 's high activity was higher than its free ligands, and that Ag(I)-L₃ had the highest activity.

SUBMITTER: Mohamed SF

PROVIDER: S-EPMC7719257 | biostudies-literature | 2020 Dec

REPOSITORIES: biostudies-literature

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Spectral, thermal, antimicrobial studies for silver(I) complexes of pyrazolone derivatives.

Mohamed Soha F SF Shehab Wesam S WS Abdullah Aboubakr M AM Sliem Mostafa H MH El-Shwiniy Walaa H WH

BMC chemistry 20201205 1

<h4>Background</h4>Synthesize new complexes of Ag(I) to enhance efficacy or stability and also, pharmacological activities on the operation of pyrazolone's biological properties.<h4>Results</h4>Efficient and high yielding pathways starting from the versatile and readily available 3-methyl-1-phenyl-5-pyrazolone by Knoevenagel condensation of a sequence of 4-arylidene-3-methyl-1-phenyl-5-pyrazolone derivatives (2a-c) have been formed by the reaction of various substituted aromatic aldehydes Used a ...[more]

PMID: 33292420

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Project description:This work describes the synthesis and characterization of three molybdenum dinitrosyl Schiff base complexes of the general formula [Mo(NO)2(L)(OH)], where L is N-(dehydroacetic acid)-4-aminoantipyrene (dha-aapH), N-(4-acetylidene-3-methyl-1-phenyl-2-pyrazolin-5-one)-4-aminoantipyrine (amphp-aapH) or N-(3-methyl-1-phenyl-4-propionylidene-2-pyrazolin-5-one)-4-aminoantipyrine (mphpp-aapH). The complexes were formulated on the basis of spectroscopic analyses, elemental composition, magnetic susceptibility measurements, molar conductance behaviour and determination of the respective decomposition temperatures. A comparative experimental-theoretical approach was followed to elucidate the structure of the complexes. Fourier transform infra-red (FT-IR) spectroscopy, thermo-gravimetry (TG) and electronic spectral insights were mainly focused on the confirmation of the formation of the complexes. The computational density functional theory (DFT) calculations evaluated in the study involve the molecular specification for the use of LANL2DZ/RB3LYP formalism for metal atoms and 6-311G/RB3LYP for the remaining non-metal atoms. The study reveals a suitable cis-octahedral geometry for the complexes. The TG curve of one of the representative complexes was evaluated to find the respective thermodynamic and kinetic parameters using various physical methods. The Freeman & Carroll (FC) differential method, the Horowitz and Metzger (HM) approximation method, the Coats-Redfern method and the Broido method were employed to present a comparative thermal analysis of the complex. The Broido method proved the best fit to the results for the compound under question. In addition to structural and thermal analyses, the study also deals with the in vitro antimicrobial and anticancer sensitivity of the complexes. The results revealed potent biological properties of the representative complex containing dha-aapH. Cell toxicity tests against COLO-205 human cancer cell line using a 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) assay showed an IC50 value of 53.13 μgm mL-1 for the Schiff base and 10.51 μgm L-1 for the respective complex. Similarly the same complex proved to be an effective antimicrobial agent against Aspergillus, Pseudomonas, E. coli and Streptococcus. The results indicated a more pronounced activity against Pseudomonas and Streptococcus than the other two microbial species.

Project description:BACKGROUND:Public health systems today face the dual challenges of controlling infections and curbing the increase in antimicrobial resistance manifested in drug-resistant microorganisms in hospitals and elsewhere. In the last ten years, research has been conducted to develop new materials with antimicrobial properties to be used in medical devices, increasingly found to harbour critical nosocomial infections. METHODS:Two next-generation composites using the antimicrobial qualities of silver were tested against Escherichia coli, Staphylococcus aureus and Candida albicans with the purpose of evaluating their antimicrobial and antifungal activity. These tests applied the standardized method according to ISO-2216: Plastics-Measurement of Antibacterial Activity on Plastics Surfaces. Testing was carried out using polyethylene (PE) enriched with AgNO3 as a positive control and PE as a negative control. RESULTS:The antimicrobial activity of the composites proved to be between medium (bacteriostatic) and very good (bactericidal). In particular, PE2 showed the highest scores against all microorganisms, with values ranging from good to very good. Instead, PE1 had lower scores, with a value of medium for Escherichia coli and slight for Candida albicans. Statistical analysis carried out with the t-test for unpaired data showed a statistically significant difference between the positive control and the other polymers (p< .0001). CONCLUSIONS:Based on our findings, we conclude that the test, conducted to ISO-2216 standards, could be extended to include fungal strains and that the new composites could be used to produce antimicrobial surfaces for medical devices, for example, intubation tubes, urinary catheters, vascular prostheses, and mechanical heart valves. This would reduce the risk of microbial contamination and biofilm formation, ensuring better health outcomes for patients treated with these devices. Further testing should be done to evaluate potential future applications of these composites and the possibility of adding fungal strains to the IS0-2216 standard.

Dataset Information

Spectral, thermal, antimicrobial studies for silver(I) complexes of pyrazolone derivatives.

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Spectral, thermal, antimicrobial studies for silver(I) complexes of pyrazolone derivatives.

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