The unprecedented polymorphism of the non-steroidal anti-inflammatory drug (NSAID) flufenamic acid (FFA) is described here. Nine polymorphs were accessed through the use of polymer-induced heteronucleation (PIHn) and solid-solid transformation at low temperature. Structural elucidation of six of these forms, in addition to the two previously known forms, makes FFA indisputably octamorphic. Although the structure of at least one other form of FFA remains elusive, the occurrence of most of these polymorphs under one crystallization condition through PIHn illustrates that a fine interplay exists among the kinetic factors that lead to phase selection in this NSAID.
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http://dx.doi.org/10.1021/ja302601f | DOI Listing |
Adv Med Sci
January 2025
Department of Histology and Embryology, Faculty of Medicine, Collegium Medicum in Bydgoszcz, Nicolaus Copernicus University in Toruń, Toruń, Poland; Faculty of Medicine, Collegium Medicum, Mazovian Academy in Płock, Płock, Poland.
Purpose: Proper functioning of the endothelial barrier is crucial for cardiovascular system homeostasis. Oxidative stress can lead to endothelial dysfunction (ED), damaging lipids, proteins, and DNA. Reactive oxygen species also increase cytoplasmic Ca levels, activating transient receptor potential melastatin 2 (TRPM2), a membrane non-selective calcium channel.
View Article and Find Full Text PDFInt J Mol Sci
December 2024
Department of General and Inorganic Chemistry, Faculty of Chemistry, Aristotle University of Thessaloniki, GR-54124 Thessaloniki, Greece.
Nine manganese(II) complexes with a series of non-steroidal anti-inflammatory drugs (namely sodium diclofenac, diflunisal, flufenamic acid, sodium meclofenamate, mefenamic acid, and tolfenamic acid) were prepared in the presence of diverse nitrogen donors, i.e., pyridine, 1,10-phenanthroline, 2,2'-bipyridine and neocuproine, as co-ligands and were characterized with spectroscopic techniques and single-crystal X-ray crystallography.
View Article and Find Full Text PDFBiochemistry
January 2025
Division of Food Science and Biotechnology, Graduate School of Agriculture, Kyoto University, Sakyo-ku, Kyoto 606-8502, Japan.
CYP105A1 exhibits monooxygenase activity to a wide variety of structurally different substrates with regio- and stereospecificity, making its application range broad. Our previous studies have shown that CYP105A1 wild type and its variants metabolize 12 types of nonsteroidal anti-inflammatory drugs (NSAIDs). In particular, the R84A variant exhibited a high activity against many NSAIDs.
View Article and Find Full Text PDFJ Colloid Interface Sci
December 2024
Department of Chemical Sciences, SSPC, the Research Ireland Centre for Pharmaceuticals, Bernal Institute, University of Limerick, V94 T9PX, Ireland. Electronic address:
Hypothesis: It is hypothesised in this work that mesoscale clusters will be present in both undersaturated and supersaturated solutions of organic pharmaceutical molecules. These clusters, being loose aggregates, could be sensitive to shear forces experienced during filtration. Thus, comparing the behaviour of these clusters alongside nanoparticles during filtration-an important sample treatment parameter during crystallization-will elucidate qualitative differences from solid, crystalline nanoparticles of similar size.
View Article and Find Full Text PDFChem Commun (Camb)
December 2024
Department of Medicinal Chemistry, Uppsala University, 751 23 Uppsala, Sweden.
A new functional group transformation allowing the synthesis of methyl-dithioesters from readily available trifluoromethyl arenes defluorinative functionalization has been developed. This microwave-assisted method is operationally simple, rapid, and eliminates the need for pre-functionalization while accommodating a broad range of functional groups. In addition, it does not rely on highly odorous thiol sources, and utilizes the commercially available reagent BFSMe complex as a multifunctional Lewis acid/sulfur source/defluorination and demethylation agent.
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