Exploration of the structure-activity relationships of the traditional C-5 acetamidomethyl side chain of the oxazolidonone antibacterials has yielded new, potent series of compounds of which the first examples, the O-linked iosoxazoles are described in detail, leading to the selection of the pre-clinical candidate AZD2563.
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http://dx.doi.org/10.1016/j.bmcl.2003.07.033 | DOI Listing |
Mol Divers
January 2025
Department of Laboratory Medicine, The Fourth People's Hospital of Nanhai District of Foshan City, Foshan, 528000, Guangdong, China.
Disruption of the mycobacterial redox homeostasis leads to irreversible stress induction and cell death. Hydroquinone scaffolds, as a new type of redox cycling anti-tuberculosis chemotypes, exhibit potent bactericidal activity against non-replicating, nutrient-deprived phenotypically drug-resistant bacteria. Evidences from microbiological, biochemical, and genetic studies indicate that the redox-driven mode of action relies on the reduction of quinones by type II NADH dehydrogenase (NDH2), generating reactive oxygen species (ROS) of bactericidal level.
View Article and Find Full Text PDFMol Divers
January 2025
Department of Microbiology, Maharshi Dayanand University, Rohtak, Haryana, 124001, India.
Cyclotides are a class of plant-derived cyclic peptides having a distinctive structure with a cyclic cystine knot (CCK) motif. They are stable molecules that naturally play a role in plant defense. Till date, more than 750 cyclotides have been reported among diverse plant taxa belonging to Cucurbitaceae, Violaceae, Rubiaceae, Solanaceae, and Fabaceae.
View Article and Find Full Text PDFPathogens
January 2025
Research and Production Center for Microbiology and Virology, Almaty 050010, Kazakhstan.
While studying the prevalence and profile of antibiotic resistance among isolated from the feces of calves with signs of colibacillosis, a strain with a wide spectrum of drug resistance was isolated. Whole-genome sequencing, followed by bioinformatic processing and the annotation of genes of this strain, showed that the genome has a total length of 4,803,482 bp and contains 4986 genes, including 122 RNA genes. A total of 31% of the genes are functionally significant and represent 26 functional groups.
View Article and Find Full Text PDFMolecules
January 2025
Institute of Bioorganic & Medicinal Chemistry, Key Laboratory of Applied Chemistry of Chongqing Municipality, School of Chemistry and Chemical Engineering, Southwest University, Chongqing 400715, China.
The overprescription of antibiotics in medicine and agriculture has accelerated the development and spread of antibiotic resistance in bacteria, which severely limits the arsenal available to clinicians for treating bacterial infections. This work discovered a new class of heteroarylcyanovinyl quinazolones and quinazolone pyridiniums to surmount the increasingly severe bacterial resistance. Bioactive assays manifested that the highly active compound exhibited strong inhibition against MRSA and with extremely low MICs of 0.
View Article and Find Full Text PDFMicroorganisms
January 2025
Department of Molecular Biology, Faculty of Biology, University of Plovdiv, Tzar Assen 24, 4000 Plovdiv, Bulgaria.
Lactobacillus is a key genus of probiotics commonly utilized for the treatment of oral infections The primary aim of our research was to investigate the probiotic potential of the newly isolated DPL5 strain from human breast milk, focusing on its ability to combat biofilm-forming pathogens such as . Employing in vitro approaches, we demonstrate DPL5's ability to endure at pH 3 with survival rates above 30%, and withstand the osmotic stress often found during industrial processes like fermentation and freeze drying, retaining over 90% viability. The lyophilized cell-free supernatant of DPL5 had a significant antagonistic effect against biofilm-producing nasal strains of , and it completely eradicated biofilms at subinhibitory concentrations of 20 mg·mL.
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