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6-Bromoindole- and 6-Bromoindazole-Based Inhibitors of Bacterial Cystathionine γ-Lyase Containing 3-Aminothiophene-2-Carboxylate Moiety.
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January 2025
Engelhardt Institute of Molecular Biology of the Russian Academy of Sciences, 32 Vavilov St., Moscow 119991, Russia.
In recent years, a number of synthetic potentiators of antibiotics have been discovered. Their action can significantly enhance the antibacterial effect and limit the spread of antibiotic resistance through inhibition of bacterial cystathionine-γ-lyase. To expand the known set of potentiators, we developed methods for the synthesis of five new representatives of 6-bromoindole derivatives-potential inhibitors of bacterial cystathionine-γ-lyase-namely potassium 3-amino-5-((6-bromoindolyl)methyl)thiophene-2-carboxylate () and its 6-bromoindazole analogs ( and ), along with two 6-broindazole analogs of the parent compound .
View Article and Find Full Text PDFAdvanced Large-Stokes-Shift Fluorescent Probe for the Detection of Biothiols: Facilitating Accurate Indirect Measurement of β-Lactamases.
Int J Mol Sci
January 2025
College of Pharmacy, Qiqihar Medical University, Qiqihar 161006, China.
A novel fluorescent probe, Bibc-DNBS, based on the combination of the PET (photoinduced electron transfer) and ESIPT (excited-state intramolecular proton transfer) mechanisms, was designed and synthesized. Bibc-DNBS exhibited a Stokes shift of 172 nm in the fluorescence detection field. In addition, the probe exhibited good performance in key parameters in bioassays such as sensitivity, specificity, and response time.
View Article and Find Full Text PDFMolecular Characterization, Recombinant Expression, and Functional Analysis of Carboxypeptidase B in .
Genes (Basel)
January 2025
CAS Key Laboratory of Tropical Marine Bio-Resources and Ecology, South China Sea Institute of Oceanology, Chinese Academy of Sciences, Guangzhou 510301, China.
The Pacific white shrimp () is economically significant, and its growth is regulated by multiple factors. Carboxypeptidase B (CPB) is related to protein digestion, but its gene sequence and features in are not fully understood. This study aimed to explore the molecular and functional properties of CPB in .
View Article and Find Full Text PDFDiscovery and Characterization of Two Selective Inhibitors for a Mu-Class Glutathione S-Transferase of 25 kDa from Using Computational and Bioinformatics Tools.
Biomolecules
December 2024
Departmento de Química, Universidad Autónoma Metropolitana-Iztapalapa, Mexico City C.P. 09310, Mexico.
Glutathione S-transferases (GSTs) are promising pharmacological targets for developing antiparasitic agents against helminths, as they play a key role in detoxifying cytotoxic xenobiotics and managing oxidative stress. Inhibiting GST activity can compromise parasite viability. This study reports the successful identification of two selective inhibitors for the mu-class glutathione S-transferase of 25 kDa (Ts25GST) from , named and , using a computationally guided approach.
View Article and Find Full Text PDFHigh prevalence of multidrug resistant and extended-spectrum β-lactamase-producing Escherichia coli and Klebsiella pneumoniae isolated from urinary tract infections in the West region, Cameroon.
BMC Infect Dis
January 2025
Department of Microbiology, Hematology and Immunology, Faculty of Medicine and Pharmaceutical Sciences, University of Dschang, Dschang, Cameroon.
Background: Antimicrobial resistance remains a worldwide health problem with serious societal and economical repercussions. Multidrug resistant and Extended-Spectrum β-Lactamase producing-Enterobacterales (ESBL-E) are pathogens of critical public health priority that urgently require the research and development of new drugs. This study aims to determine the prevalence and characterize the genes conferring resistance to β-lactams among Escherichia coli and Klebsiella pneumoniae isolated from patients with urinary tract infections (UTIs) in the West region, Cameroon.
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