Reactive oxygen and nitrogen species (RONS) contribute to the pathogenesis of neurodegeneration, but the inability to detect RONS in vivo in the central nervous system has confounded the interpretation of results of clinical trials of antioxidants. Here we report the synthesis and characterization of a positron emission tomography (PET) probe, [F]fluoroedaravone ([F]FEDV), for the in vivo quantification of oxidative stress. Derived from the antioxidant edaravone, the probe can diffuse through the blood-brain barrier and is stable in human plasma.
View Article and Find Full Text PDFBeclomethasone dipropionate (1) is a synthetic corticosteroid with anti-inflammatory, antipruritic, and anti-allergy properties. It is widely used to treat asthma, allergic rhinitis, and dermatoses. However, existing synthetic routes to this active pharmaceutical ingredient (API) contain steps resulting in low and/or inconsistent yields, and use obsolete reagents.
View Article and Find Full Text PDFDiscovering therapeutic agents: New bioactive agents, either as sole or combinational agents, have been constructed through the synthetic manipulation of the intermediates within the total synthesis of the uvaretin class of natural products. It was found that increasing the hydrophobic character of the phenolic core correlates to a decrease in sole agent cytotoxicity. The synthesis of new, small chemical screening libraries (CSL) constructed from the intermediates of our total synthesis route of the uvaretin class of natural products is demonstrated herein.
View Article and Find Full Text PDFDuring the last three decades, studies of linamarin extracted from cassava have received increased attention due to the presence of high cyanogenic compounds in these extracts. The methods that are utilized to isolate linamarin are either tedious or use acidic conditions resulting in poor yields. In this study, a novel cryocooled method of extraction has been developed to isolate linamarin from Cassava root peel.
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