Experiments on mice and rats were made to study the effect of inhibitors-antioxidants (3-hydroxypyridine derivatives) on the central nervous system. It was established that 3-hydroxypyridine derivatives (50 to 200 mg/kg) possess a broad spectrum of psychotropic effects. They cause normalization of behavior in conflict situations, exert an antiaggressive and anticonvulsant action (antagonism with corazol), are capable of potentiating the hypnotic effect of barbiturates, and of suppressing the animals' motor activity if given in high doses. Most compounds under study have antihypoxic and antiamnestic effects.
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J Hazard Mater
January 2025
Laboratory of Toxicant Analysis, Academy of Military Medical Sciences, Beijing 100850, China. Electronic address:
Organophosphorus nerve agents (OPNAs) are highly lethal chemical warfare agents (CWAs), which poses a serious threat to human health and safety. The accurate and rapid identification of OPNAs is crucial for medical diagnosis and effective treatment. However, distinguishing between various OPNAs and their analogues using on-site point-of-care testing (POCT) remains challenging.
View Article and Find Full Text PDFHeliyon
August 2024
Department of Medicinal Chemistry, Faculty of Pharmacy, Shiraz University of Medical Sciences, Shiraz, Iran.
In the present study, ten new substituted 3-hydroxypyridine-4-one derivatives were synthesized in a four-step method, and their chemical structures were confirmed using various spectroscopic techniques. Subsequently, the inhibitory activities of these derivatives against tyrosinase enzyme and their antioxidant activities were evaluated. Amongest the synthesized compounds, bearing a 4-OH-3-OCH substitution was found to be a promising tyrosinase inhibitor with an IC value of 25.
View Article and Find Full Text PDFPhys Chem Chem Phys
August 2024
G.A. Krestov Institute of Solution Chemistry of the Russian Academy of Sciences, 1 Akademicheskaya St., Ivanovo, 153045, Russian Federation.
The saturated vapour pressures of five heterocyclic compounds containing the pyridine fragment, namely, three isomers of aminopyridine (2-aminopyridine (2AmPy), 3-aminopyridine (3AmPy), and 4-aminopyridine (4AmPy)); 3-hydroxypyridine (3OHPy) and 2-(1-imidazol-2-yl)pyridine (ImPy), were measured at appropriate temperature intervals using a transpiration (inert gas flow) method. The standard molar enthalpies, entropies, and Gibbs energies of sublimation for all the studied substances were determined. Among the compounds studied, the largest value of Δ298sub was observed for ImPy.
View Article and Find Full Text PDFMed Chem
October 2024
Department of Medicinal Chemistry, Faculty of Pharmacy, Shiraz University of Medical Sciences, Shiraz, Iran.
Introduction: Drug resistance to existing antimicrobial drugs has become a serious threat to human health, which highlights the need to develop new antimicrobial agents.
Methods: In this study, a new set of 3-hydroxypyridine-4-one derivatives (6a-j) was synthesized, and the antimicrobial effects of these derivatives were evaluated against a variety of microorganisms using the microdilution method. The antimicrobial evaluation indicated that compound 6c, with an electron-donating group -OCH at the meta position of the phenyl ring, was the most active compound against and species with an MIC value of 32 μg/mL.
Bioorg Med Chem
May 2024
College of Pharmaceutical Science, Zhejiang University of Technology, Hangzhou, China; Collaborative Innovation Center of Yangtze River Delta Region Green Pharmaceutical, Zhejiang University of Technology, Hangzhou, China; Key Laboratory for Green Pharmaceutical Technologies and Related Equipment of Ministry of Education, Key Laboratory of Pharmaceutical Engineering of Zhejiang Province, Hangzhou, China. Electronic address:
5-Aminolevulinic acid (ALA) and its derivatives, serving as the endogenous precursor of the photosensitizer (PS) protoporphyrin IX (PpIX), successfully applied in tumor imaging and photodynamic therapy (PDT). ALA and its derivatives have been used to treat actinic keratosis (AK), basal cell carcinoma (BCC), and improve the detection of superficial bladder cancer. However, the high hydrophilicity of ALA and the conversion of PpIX to heme have limited the accumulation of PpIX, hindering the efficiency and potential application of ALA-PDT.
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