Different N-substituted benzisoselenazol-3(2H)-ones, analogues of ebselen were designed as new antiviral and antimicrobial agents. We report their synthesis, chemical properties as well as study on biological activity against broad spectrum of pathogenic microorganisms (Staphylococcus aureus, Staphylococcus simulans, Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoniae, Candida albicans, Aspergillus niger) and viruses (herpes simplex virus type 1 (HSV-1), encephalomyocarditis virus (EMCV), vesicular stomatitis virus (VSV)), in vitro. Most of them exhibited high activity against viruses (HSV-1, EMCV) and gram-positive bacteria strains (S. aureus, S. simulans), while their activity against gram-negative bacteria strains (E. coli, P. aeruginosa, K. pneumoniae) was substantially lower. Some of tested compounds were active against yeast C. albicans and filamentous fungus A. niger.
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http://dx.doi.org/10.1248/cpb.56.1423 | DOI Listing |
Malar J
January 2025
Department of Pharmacology, Kangwon National University School of Medicine, Chuncheon, 24341, Republic of Korea.
Background: The Plasmodium proteasome emerges as a promising target for anti-malarial drug development due to its potential activity against multiple life cycle stages.
Methods: In this investigation, a comparative analysis was conducted on the structural features of the β5 subunit in the 20S proteasomes of both Plasmodium and humans.
Results: The findings underscore the structural diversity inherent in both proteasomes.
Environ Technol
January 2025
College of Architecture & Civil Engineering, Beijing University of Technology, Beijing, People's Republic of China.
The release of algal organic matter (AOM) during seasonal algal blooms increases the complexity and heterogeneity of natural organic matter (NOM) in water sources, altering its hydrophilic-hydrophobic balance and posing significant challenges to conventional water treatment processes. This study aims to verify whether the (Granular activated carbon) GAC selected for the adsorption of NOM in sand filtration effluent can adapt to water quality fluctuations caused by AOM release, and identify the criteria influencing GAC adsorption performance. Results indicated that external surface area, mesopore volume, pore size and surface functional groups were key indicators of GAC adsorption performance.
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January 2025
Department of Clinical Pharmacy, University of Medicine and Pharmacy of Craiova, 200349, Craiova, Romania.
Cancer remains the second leading cause of death globally, driving the need for innovative therapies. Among natural compounds, maytansinoids have shown significant promise, contributing to nearly 25% of recently approved anticancer drugs. Despite their potential, early clinical trials faced challenges due to severe side effects, prompting advancements in delivery systems such as antibody-maytansinoid conjugates (AMCs).
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January 2025
Laboratory of Molecular Chemistry, Department of Chemistry, Faculty of Sciences Semlalia, Cadi Ayyad University, BP 2390, 40000, Marrakech, Morocco.
TMPRSS4, a transmembrane serine protease type II, is associated with various pathological illnesses. It has been found to activate SARS-CoV-2, enhance viral infection of human small-intestinal enterocytes and is overexpressed in different types of cancers. Therefore, this study aims to disover potential TMPRSS4 inhibitors that have better binding affinity than the approved inhibitors: 2-hydroxydiarylamide and tyroserleutide.
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January 2025
Economic Entomology Department, Faculty of Agriculture, Mansoura University, Mansoura, 35516, Egypt.
The continual use of synthetic insecticides to control mosquito larvae has severe implications for human health and the ecosystem, highlighting the need for alternative natural insecticides. Macroalgae may be a good alternative because of their biologically active metabolites with distinctive chemical structures that have been reported for their insecticidal properties. The study aimed to investigate the potential of different extracts from Jania rubens (Linnaeus) J.
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