Antimicrobial activity of 25 new original 2-aryliden-6-furfuryliden cyclohexanones and hexahydroindazoles based on them was studied. The majority of the compounds had low or moderate activity against the test cultures of Staphylococcus spp., Pseudomonas aeruginosa, Proteus spp. and Escherichia coil. Compound XIX (2,3-diphenyl-7-(5-nitrofurfuryliden)-3,3a,4,5,6,7-hexahydroindazole) with high antistaphylococcal activity was selected among several 2-aryliden-6-furfuryliden cyclohexanones and hexahydroindazoles. The activity of compound XIX was tested with the use of 105 clinical isolates of staphylococci. Comparative antistaphylococcal activity of compound XIX, furazolidone and sodium cefotaxime against the isolates was estimated. The impact of the microbial load, pH of the nutrient medium and the presence of 1%, 5% or 10% of serum or blood in the medium on the antimicrobial activity of compound XIX was evaluated. The results are in favour of further research on compound XIX as a potential agent of etiotropic therapy for staphylococcal infection.
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Int J Mol Sci
July 2024
Institute of Pharmaceutical Chemistry, University of Pécs, H-7624 Pécs, Hungary.
Non-enzyme-catalyzed thiol addition onto the α,β-unsaturated carbonyl system is associated with several biological effects. Kinetics and diastereoselectivity of non-enzyme catalyzed nucleophilic addition of reduced glutathione (GSH) and N-acetylcysteine (NAC) to the six-membered cyclic chalcone analogs and were investigated at different pH values (pH 3.2, 7.
View Article and Find Full Text PDFBiotechnol Bioeng
August 2024
Department of Chemical and Biomolecular Engineering, University of Houston, Houston, Texas, USA.
Governments and biopharmaceutical organizations aggressively leveraged expeditious communication capabilities, decision models, and global strategies to make a COVID-19 vaccine happen within a period of 12 months. This was an unusual effort and cannot be transferred to normal times. However, this focus on a single vaccine has also led to other treatments and drug developments being sidelined.
View Article and Find Full Text PDFPlants (Basel)
March 2023
Thrombosis Research Center, Medical Technology School, Department of Clinical Biochemistry and Immunohematology, Faculty of Health Sciences, Universidad de Talca, Talca 3480094, Chile.
Aqueous and ethanolic extracts of tomato pomace were examined with the aim of optimizing the extraction process of compounds with cardioprotective activity. Once the results of the ORAC response variables, total polyphenols, °Brix, and antiplatelet activity of the extracts were obtained, a multivariate statistical analysis was performed using the Statgraphics Centurion XIX software. This analysis showed that the most relevant positive effects in the inhibition of platelet aggregation were 83 ± 2% when using the agonist TRAP-6, when the working conditions were the type of tomato pomace conditioning (drum-drying process at 115 °C), phase ratio (1/8), type of solvent (ethanol 20%), and type of extraction (ultrasound-assisted solid-liquid extraction).
View Article and Find Full Text PDFMolecules
February 2023
Department of Biology, Ecology and Earth Sciences DIBEST, University of Calabria, Via Pietro Bucci, Arcavacata, 87036 Rende, Italy.
Over the centuries, humans have developed different systems to protect surfaces from the influence of environmental factors. Protective paints are the most used ones. They have undergone considerable development over the years, especially at the turn of the 19th and 20th centuries.
View Article and Find Full Text PDFPharmaceutics
August 2022
Institute of Exact and Natural Sciences, Federal University of Pará, Augusto Corrêa, 01, Guamá, Belém 66075-110, PA, Brazil.
L. (Cucurbitaceae) is a plant known in Brazil as "melão de São Caetano", which has been related to many therapeutic applications in folk medicine. Herein, we describe antibacterial activities and related metabolites for an extract and fractions obtained from the leaves of that species.
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