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Here we describe a rapid and divergent synthetic route toward structurally novel αHTs functionalized with either one or two thioether or sulfonyl appendages. Evaluation of this library against hepatitis B and herpes simplex virus, as well as the pathogenic fungus , and a human hepatoblastoma (HepDES19) revealed complementary biological profiles and new lead compounds with sub-micromolar activity against each pathogen.
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http://dx.doi.org/10.1039/c9ra06383h | DOI Listing |
J Agric Food Chem
September 2025
College of Materials and Chemistry & School of Plant Protection, Anhui Agricultural University, Hefei, 230036, P. R. China.
In recent years, the hydrazide skeleton, as a pivotal class of nitrogen-containing structures, has garnered considerable attention in medicinal chemistry and organic synthesis owing to its unique chemical versatility and broad-spectrum biological activities. In this study, a series of thiazole-containing benzoylhydrazine derivatives -, -, and - with structural divergence from conventional hydrazide-based molecular frameworks were designed, synthesized, and evaluated for their antifungal/antioomycete activities. The antifungal/antioomycete assay showed that some of the targeted compounds exhibited remarkable and broad-spectrum antifungal activities.
View Article and Find Full Text PDFOrg Lett
September 2025
School of Chemistry and Chemical Engineering, Guangxi Colleges and Universities Key Laboratory of Applied Chemistry Technology and Resource Development, Guangxi University, Nanning 530004, China.
Vinylphosphonates serve as crucial components in synthetic chemistry, medicinal chemistry, and materials science. However, traditional synthetic methods for these compounds typically require the use of noble metal catalysts and hazardous reagents. Herein, we report a metal-free strategy for the divergent synthesis of vinylphosphonates through the P nucleophilic addition of vinylidene -quinone methides (-VQMs).
View Article and Find Full Text PDFJ Am Chem Soc
September 2025
Department of Chemistry, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037, United States.
Diversity-oriented synthesis (DOS) has emerged as an efficient strategy for constructing diverse compound libraries, facilitating hit or lead identification in the drug discovery process. In parallel, developing diverse transformations at different sites is an appealing strategy to expand the diversity of appendages on scaffolds. Owing to the availability of C-H bonds at multiple sites of pharmacophores, diversity-oriented C-H activation reactions are an ideal approach to realize this goal.
View Article and Find Full Text PDFScand J Med Sci Sports
September 2025
Department of Biomedical Sciences, Faculty of Health and Medical Sciences, University of Copenhagen, Copenhagen, Denmark.
Dietary intake has an important influence on rates of fuel use during exercise, but the extent to which short-term diet changes affect peak fat oxidation (PFO) and the intensity at which this occurs (Fat) is unknown. This study examined the impact of diet-induced changes in substrate availability on PFO and Fat and the expression of key lipid-regulatory genes and proteins in skeletal muscle. Forty moderately to well-trained males (27 ± 5 years, V̇O 56.
View Article and Find Full Text PDFJ Agric Food Chem
September 2025
State Key Laboratory of Green Pesticide, Center for R&D of Fine Chemicals of Guizhou University, Guiyang 550025, China.
Structurally unique halichonine B is promising for the design of pharmaceutical leads, while function-oriented optimization is unknown in agrochemical science. Our recent practical synthesis offers a great chance for the discovery of antimicrobial leads. "Linker plus replaceable substituents" is exerted, in which up to 9 unique linkers together with diverse substituents from a wide chemical space are investigated for optimization of the readily available drimanyl amine.
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