Eighteen substituted thiophene and benzothiophene derivatives were studied for their effects on peroxisome proliferator-activated receptor gamma (PPARgamma) in HepG2 cells. Three derivatives (compounds 5, 120.97%; 15, 102.14%; and 17, 113.82%) were found to transactivate PPARgamma in vitro. By comparison, the positive control rosiglitazone (Ros) transactivated PPARgamma by 311.53%. The three compounds were studied for their effects on glucose metabolism in vivo in KK/Ay diabetic mice. In vivo, the 2-(beta-carbonyl/sulfonyl) butyryl-thiophene compounds 5 and 15 significantly decreased blood glucose levels (compounds 5, to<15.6mmol/L; 15, to<10mmol/L), improved glucose tolerance, improved impaired pancreatic islet beta-cells, and lowered serum insulin levels.
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http://dx.doi.org/10.1080/14756360903179369 | DOI Listing |
Bioorg Chem
January 2025
Chemistry Department, Faculty of Science, Ain Shams University, Abbasia, 11566 Cairo, Egypt.
The escalating prevalence of antibiotic-resistant bacteria has led to a serious global public health problem; therefore, there is an urgent need for the development of structurally innovative antibacterial agents. In our study, different series of tetra-substituted thiophene derivatives were designed and synthesized by multi-component reactions (MCRs) in moderate to excellent yields. Some of the designed final compounds were synthesized by both microwave assisted method and traditional synthesis.
View Article and Find Full Text PDFMolecules
December 2024
Institute of Organic and Analytical Chemistry (ICOA UMR 7311), CNRS, University of Orleans, F-45067 Orléans, France.
The emergence of RNA viruses driven by global population growth and international trade highlights the urgent need for effective antiviral agents that can inhibit viral replication. Nucleoside analogs, which mimic natural nucleotides, have shown promise in targeting RNA-dependent RNA polymerases (RdRps). Starting from protected 5-iodouridine, we report the synthesis of -substituted-(1,3-diyne)-uridines nucleosides and their phosphoramidate prodrugs.
View Article and Find Full Text PDFMini Rev Med Chem
January 2025
Department of Chemistry, Faculty of Science, Universiti Teknologi Malaysia, Johor Bahru 81310, Johor, Malaysia.
Indole, a ubiquitous structural motif in bioactive compounds, has played a pivotal role in drug discovery. Among indole derivatives, indole-3-carboxaldehyde (I3A) has emerged as a particularly promising scaffold for the development of therapeutic agents. This review delves into the recent advancements in the chemical modification of I3A and its derivatives, highlighting their potential applications in various therapeutic areas.
View Article and Find Full Text PDFMaterials (Basel)
December 2024
Flinders Institute for NanoScale Science and Technology, College of Science and Engineering, Flinders University, Sturt Road, Bedford Park, Adelaide, SA 5042, Australia.
In recent years, the design and synthesis of high-performing conjugated materials for the application in organic photovoltaics (OPVs) have achieved lab-scale devices with high power conversion efficiency. However, most of the high-performing materials are still synthesised using complex multistep procedures, resulting in high cost. For the upscaling of OPVs, it is also important to focus on conjugated polymers that can be made via fewer simple synthetic steps.
View Article and Find Full Text PDFJ Biol Inorg Chem
December 2024
Izmir International Biomedicine and Genome Institute, Dokuz Eylul University, 35340, Izmir, Turkey.
As novel promising anticancer candidates, the piano-stool type complexes of ruthenium, [RuCl(η-p-cymene)(N,S-L)]PF, K-, were synthesized from the reaction of the substituted benzo[b]thiophene based thiosemicarbazone ligands (L) with [{RuCl(η-p-cymene)}(μ-Cl)]. All complexes were fully characterized using elemental analysis, and spectroscopic methods such as FT-IR and H NMR. The molecular masses of the complexes were proved by MALDI-TOF analysis.
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