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Pyrazole derivatives are aromatic heterocyclic compounds endowed with multifaceted applications. In the present study 1,3,4-trisubstituted pyrazoles derivatives have been synthesized for the purpose of studying their physical properties and their characterization was done by FTIR, H NMR and C NMR spectroscopic technique. The measurement of densities (ρ) and viscosities (η) of solutions of substituted pyrazole derivative in polar aprotic solvent i.e., Dimethyl sulfoxide (DMSO), nitromethane (NM) as well as in their 1:1 binary mixture (DMSO + NM) was done at 310 K over a wide range of solute concentration (5-100) × 10 mol dm. The experimental results were used to determine the excess molar volumes . The data of density-viscosity revealed the dipole-dipole interactions occurred between the pyrazole derivative (solute) and the solvent (DMSO, NM). Excess molar studies revealed that solute-solvent interaction was found to be stronger in case of nitromethane solvent.
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http://dx.doi.org/10.1038/s41598-024-69167-z | DOI Listing |
Anal Methods
September 2025
Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia.
Avapritinib (Ayvakit™) is a highly selective inhibitor of the platelet-derived growth factor receptor alpha (PDGFRA), including D842V mutations. Avapritinib (APB) is authorized in the United States for individuals with metastatic or unresectable gastrointestinal stromal tumors (GISTs). APB is considered the exclusive therapy for adults with indolent systemic mastocytosis.
View Article and Find Full Text PDFCurr Med Chem
September 2025
Laboratory of Molecular Basis of Action of physiologically active compounds, Engelhardt Institute of Molecular Biology, Russian Academy of Sciences, 119991, Moscow, Russia.
Introduction: Chemotherapy remains essential despite advances in immunotherapy, radiotherapy, and biological therapy. However, the wide range of chemical drugs is limited by a narrow therapeutic index, low selectivity, and the development of resistance. In this regard, new high-efficiency drugs are in extremely high demand.
View Article and Find Full Text PDFbioRxiv
August 2025
Department of Chemistry, University of Alberta, Edmonton, AB T6G 2G2, Canada.
Genetically-encoded libraries of peptide-derived macrocycles containing electrophile 'warheads' (cGELs) can be used to identify potent and selective covalent ligands for protein targets. Such cGELs are synthesized either by incorporation of unnatural amino acids that display mild electrophiles on their side chains or by chemical post-translational modification (cPTM) of mRNA or phage-displayed peptide libraries. Here we investigate fundamental barriers to the synthesis of cGELs.
View Article and Find Full Text PDFCurr Top Med Chem
September 2025
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Trakya University, Edirne, Turkiye.
Org Lett
September 2025
N. D. Zelinsky Institute of Organic Chemistry, Leninsky Prospekt 47, Moscow 119991, Russian Federation.
The first radical addition to mesoionic heterocycles, enabling direct functionalization of sydnones with perfluoroalkyl groups with retention of the mesoionic structure, is described. The fluorinated sydnones were subsequently involved in the energy-transfer-mediated cycloaddition with silyl enol ethers. This approach provides efficient access to medicinally relevant perfluoroalkylated pyrazole derivatives with complete regiocontrol.
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