We explored the antibacterial potential (alone and combination) against multidrug resistant (MDR) Pseudomonas aeruginosa isolates KG-P2 using synthesized thieno[3,2-c]pyran-2-ones in combination with different antibiotics. Out of 14 compounds, two compounds (3g and 3l) abridged the MIC of tetracycline (TET) by 16 folds. Compounds was killing the KG-P2 cells, in time dependent manner, lengthened post-antibiotic effect (PAE) of TET and found decreased the mutant prevention concentration (MPC) of TET. In ethidium bromide efflux experiment, two compounds repressed the drug transporter (efflux pumps) which is further supported by molecular docking of these compounds with efflux complex MexAB-OprM. In another study, these compounds inhibited the synthesis of biofilm.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.biopha.2021.112084 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Affinity descriptor of metal catalysts: concept, measurement and application of oxygen affinity in the catalytic transformation of oxygenates.
Chem Soc Rev
January 2025
National-local Joint Engineering Research Center of Biomass Refining and High-quality Utilization, Changzhou University, Changzhou 213164, China.
Multiple oxygenate groups in biomass-based feedstocks are open to multiple catalytic pathways and products, typically resulting in low selectivity for the desired products. In this context, strategies for rational catalyst design are critical to obtain high selectivity for the desired products in biomass upgrading. The Sabatier principle provides a conceptual framework for designing optimal catalysts by following the volcanic relationship between catalyst activity for a reaction and the binding strength of a substrate on a catalyst.
View Article and Find Full Text PDFRepurposing Linezolid in Conjunction with Histone Deacetylase Inhibitor Access in the Realm of Glioblastoma Therapies.
J Med Chem
January 2025
School of Pharmacy, College of Pharmacy, Taipei Medical University, Taipei 110, Taiwan.
Since decades after temozolomide was approved, no effective drugs have been developed. Undoubtedly, blood-brain barrier (BBB) penetration is a severe issue that should be overcome in glioblastoma multiforme (GBM) drug development. In this research, we were inspired by linezolid through structural modification with several bioactive moieties to achieve the desired brain delivery.
View Article and Find Full Text PDFNano-sized heterogeneous photocatalyst FeO@V/TiO-catalyzed synthesis and antimycobacterial evaluation of 2-substituted benzimidazoles.
Mol Divers
January 2025
School of Life Sciences, Jilin University, 2699 Qianjin Street, Changchun, 130012, People's Republic of China.
The 2-substituted benzimidazole has emerged as a promising heterocyclic compound in the field of drug design. In pursuit of more sustainable photocatalysts for 2-substituted benzimidazole synthesis, the method for coating FeO with V-doped TiO was presented. On the base of characterizing composition, morphology, and properties, the prepared nano-sized FeO@V/TiO composites were used as a heterogeneous photocatalyst to catalyze the synthesis of 2-substituted benzimidazoles under light.
View Article and Find Full Text PDFSynergistic activity of Pitstop-2 and 1,6-hexanediol in aggressive human lung cancer cells.
Discov Nano
January 2025
Institute of Physiology II, University of Münster, Robert-Koch-Str. 27b, 48149, Münster, Germany.
Metastatic cancer cells undergo metabolic reprogramming, which involves changes in the metabolic fluxes, including endocytosis, nucleocytoplasmic transport, and mitochondrial metabolism, to satisfy their massive demands for energy, cell division, and proliferation compared to normal cells. We have previously demonstrated the ability of two different types of compounds to interfere with linchpins of metabolic reprogramming, Pitstop-2 and 1,6-hexanediol (1,6-HD). 1,6-HD disrupts glycolysis enzymes and mitochondrial function, enhancing reactive oxygen species production and reducing cellular ATP levels, while Pitstop-2 impedes clathrin-mediated endocytosis and small GTPases activity.
View Article and Find Full Text PDFTacrolimus and diabetic rodent models.
Pharmacol Rep
January 2025
Department of Pharmacy, The First People's Hospital of Changzhou/The Third Affiliated Hospital of Soochow University, Changzhou, 213003, Jiangsu, China.
Tacrolimus (TAC) is an immunosuppressant widely utilized in organ transplantation. One of its primary adverse effects is glucose metabolism disorder, which significantly increases the risk of diabetes. Investigating the molecular mechanisms underlying TAC-induced diabetes is essential for developing effective prevention and treatment strategies for these adverse effects.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!