4.7 Article

Glucosylated Deferiprone and Its Brain Uptake: Implications for Developing Glucosylated Hydroxypyridinone Analogues Intended to Cross the Blood-Brain Barrier

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JOURNAL OF MEDICINAL CHEMISTRY
卷 53, 期 15, 页码 5886-5889

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AMER CHEMICAL SOC
DOI: 10.1021/jm100380k

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  1. Apotex Incorporation, Canada

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This report presents that Deferiprone, the only clinically used 3-hydroxypyridin-4-one (HPO), is able to penetrate the blood-brain barrier (BBB) in guinea pigs, whereas its glucosylated analogue is unable to do so. This finding is contrary to published information suggesting that the glucosylation of HPOs is a viable means of enhancing the brain uptake of this group of compounds.

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