Emerging and reemerging viruses pose significant public health threats, underscoring the urgent need for new antiviral drugs. Recently, a novel family of antiviral acyclic nucleoside phosphonates (ANP) composed of a 4-(2,4-diaminopyrimidin-6-yl)oxy-but-2-enyl phosphonic acid skeleton (O-DAPy nucleobase) has shown promise. Among these, LAVR-289 stands out for its potent inhibitory effects against various DNA viruses.
View Article and Find Full Text PDFA molecularly imprinted polymer of Tenofovir (1), an FDA-approved acyclic nucleoside phosphonate with antiviral activity, was synthesized using a non-covalent approach. A pre-polymerization complex was formed between (1) and DMAEMA and in-house synthetic -[(2-methacryloyloxy)ethyl] thymine, with EGDMA as a cross-linker in an MeCN/HO (9:1, 1:1) mixture as a porogen, giving an imprinting factor (IF) of 5.5 at 2.
View Article and Find Full Text PDF(Re)emerging RNA viruses have been major threats to public health in the past years, and from the few drugs available, nucleoside analogues are still at the cornerstone of the antiviral therapy. Among them, the synthesis of carbocyclic -nucleosides is suffering from long syntheses and poor yields. Herein we report a concise stereoselective synthesis of rare carbocyclic -nucleosides (11a-l) bearing non-canonical nucleobases through a cobalt-assisted-route as key step starting from the optically pure (-)-cyclopentenone 1.
View Article and Find Full Text PDFThe assessment of the enteric nervous system provides a better understanding of the effects that contaminants can have on the health and well-being of organisms. It has been reported that 2,4-dichlorophenoxyacetic acid (2,4-D) is a highly persistent herbicide in the environment that is responsible for neurotoxic changes in different myenteric neuronal subpopulations. The current study aimed to evaluate the effects of 2,4-D on myenteric neurons in the colon of for the first time.
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