A new series of S-alkylisothiosemicarbazones of 3- and 4-pyridincarboxaldehyde and 4-fluoro- and 4-trifluoromethylbenzaldehyde was synthesized and evaluated for biological activity against various Mycobacterium strains. Inhibitory activity against Mycobacterium tuberculosis H37Rv ATCC 27294 and INH-R ATCC 35822 was compared with activity against clinical isolated Mycobacteria as well as against MOTT. Some of newly prepared compounds showed best inhibitory values against clinical isolated Mycobacteria, besides to low citotoxicity values.
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http://dx.doi.org/10.1016/s0968-0896(01)00310-8 | DOI Listing |
Bioorg Med Chem Lett
January 2025
Calibr-Skaggs Institute for Innovative Medicines, a division of Scripps Research, La Jolla, CA 92037, United States. Electronic address:
Screening of the ChemDiv molecular library in cholesterol media against Mycobacterium tuberculosis (Mtb) H37Rv strain identified a novel isoxazole thiophene hit as a putative Rv1625c/Cya activator with a promising in vitro activity and good pharmacokinetic properties. Twenty-nine analogs were synthesized to assess the structure-activity relationships (SAR) to further improve potency. The most notable analog was P15, which showed an intramacrophage EC = 1.
View Article and Find Full Text PDFLancet Glob Health
January 2025
Pathogenesis and Control of Chronic and Emerging Infections, University of Montpellier, Institut National de la Santé et de la Recherche Médicale, Montpellier, France. Electronic address:
People who use drugs show a higher incidence and prevalence of tuberculosis than people who do not use drugs in areas where Mycobacterium tuberculosis is endemic. However, this population is largely neglected in national tuberculosis programmes. Strategies for active case finding, screening, and linkage to care designed for the general population are not adapted to the needs of people who use drugs, who are stigmatised and difficult to reach.
View Article and Find Full Text PDFMol 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 PDFMolecules
January 2025
N. S. Kurnakov Institute of General and Inorganic Chemistry, Russian Academy of Sciences, Leninsky Prosp. 31, 119991 Moscow, Russia.
The interaction of sodium phytate hydrate CHOP·xNa·yHO (phytNa) with Cu(OAc)·HO and 1,10-phenanthroline (phen) led to the anionic tetranuclear complex [Cu(HO)(phen)(phyt)]·2Na·2NH·32HO (), the structure of the latter was determined by X-ray diffraction analysis. The phytate is completely deprotonated; six phosphate fragments (with atoms P1-P6) are characterized by different spatial arrangements relative to the cyclohexane ring (1a5e conformation), which determines two different types of coordination to the complexing agents-P1 and P3, P4, and P6 have monodentate, while P2 and P5 are bidentately bound to Cu cations. The molecular structure of the anion complex is stabilized by a set of strong intramolecular hydrogen bonds involving coordinated water molecules.
View Article and Find Full Text PDFMicroorganisms
January 2025
Department of Biology, College of Science and Math, California State University, Northridge, CA 91330, USA.
The fungal genus is noted for its bioluminescence and the production of biologically active secondary metabolites. We isolated 47 fungal strains of germinated from spores of a single mushroom. We first noted a high degree of variation in the outward appearances in radial growth and pigmentation among the cultures.
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