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Sulphonyl thiourea compounds containing pyrimidine as dual inhibitors of I, II, IX, and XII carbonic anhydrases and cancer cell lines: synthesis, characterization and studies.
RSC Med Chem
December 2024
VNU University of Education, Vietnam National University, Hanoi 144 Xuan Thuy, Cau Giay Ha Noi Vietnam.
Some novel sulphonyl thiourea derivatives (7a-m) containing 4,6-diarylpyrimidine rings were designed and synthesized using a one-pot procedure. These compounds exhibited remarkable dual inhibitory activity against human carbonic anhydrase CA I, CA II, CA IX, and XII isoenzymes and some cancer cell lines. Among them, some thioureas had significantly more potent inhibitory activities in the order of 7l > 7c > 7f (against the CA I isoform), 7f > 7b > 7c (against the CA II isoform), 7c > 7g > 7a > 7b (against the CA IX isoform), and 7d > 7c > 7g > 7f (against the CA XII isoform).
View Article and Find Full Text PDFPreclinical and in silico studies of 3-benzothioyl-1-(3-hydroxy-3-phenyl-3-propyl)-1-methylthiourea: a promising agent for depression and anxiety.
Eur J Pharmacol
January 2025
Department of Pharmacy, Abdul Wali Khan University Mardan, Mardan-23200, Pakistan; Department of Pharmacy, Korea University, Sejong 20019, South Korea. Electronic address:
The study investigated the anxiolytic, antidepressant, sedative/hypnotic and in silico molecular docking properties of the synthetic ephedrine-based derivative of thiourea, 3-benzothioyl-1-(3-hydroxy-3-phenyl-3-propyl)-1-methylthiourea. Safety profile of the compound at various doses was determined in an acute toxicity test. Results showed significant anti-anxiety effects of the compound in all mice studies.
View Article and Find Full Text PDFRadiolytic Elimination of Nabumetone from Aqueous Solution: Degradation Efficiency, and Degradants' Toxicity.
Molecules
December 2024
Department of Chemistry, Faculty of Science, University of Zagreb, Horvatovac 102a, 10000 Zagreb, Croatia.
Advanced oxidation processes (AOPs), including ionizing radiation treatment, are increasingly recognized as an effective method for the degradation of pharmaceutical pollutants, including non-steroidal anti-inflammatory drugs (NSAIDs). Nabumetone (NAB), a widely used NSAID prodrug, poses an environmental risk due to its persistence in aquatic ecosystems and its potential toxicity to non-target organisms. In this study, the radiolytic degradation of NAB was investigated under different experimental conditions (dose rate, radical scavenging, pH, matrix effect), and the toxicity of its degradation products was evaluated.
View Article and Find Full Text PDFSynthesis and Structure-Activity Relationship of Thiourea Derivatives Against .
Pharmaceuticals (Basel)
November 2024
Laboratório de Bioquímica de Tripanosomatídeos, Instituto Oswaldo Cruz, Fundação Oswaldo Cruz, Rio de Janeiro 21040-900, Brazil.
Leishmaniasis, caused by protozoa and transmitted by vectors, presents varied clinical manifestations based on parasite species and host immunity. The lack of effective vaccines or treatments has prompted research into new therapies, including thiourea derivatives, which have demonstrated antiprotozoal activities. We synthesized two series of ,'-disubstituted thiourea derivatives through the reaction of isothiocyanates with amines.
View Article and Find Full Text PDFEco-Friendly Synthesis of Quinazoline Derivatives Through Visible Light-Driven Photocatalysis Using Curcumin-Sensitized Titanium Dioxide.
Materials (Basel)
December 2024
Department of Chemistry, College of Science and Humanities in Al-Kharj, Prince Sattam Bin Abdulaziz University, P.O. Box 173, Al-Kharj 11942, Saudi Arabia.
This study explores a sustainable method for synthesizing quinazoline derivatives through visible light-driven photocatalysis using curcumin-sensitized titanium dioxide (TiO) nanoparticles. A one-pot, three-component reaction involving aldehydes, urea/thiourea, and dimedone was utilized to efficiently produce quinazoline compounds. The photocatalytic performance of curcumin-sensitized TiO (Cur-TiO) was compared to pure TiO (P-TiO), with Cur-TiO showing significantly enhanced activity.
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