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Design, synthesis and biological evaluation of brain-specific glucosyl thiamine disulfide prodrugs of naproxen

W Fan, Y Wu, XK Li, N Yao, X Li, YG Yu…

文献索引:Fan, Wei; Wu, Yong; Li, Xian-Kun; Yao, Nian; Li, Xun; Yu, Yong-Guo; Hai, Li European Journal of Medicinal Chemistry, 2011 , vol. 46, # 9 p. 3651 - 3661

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被引用次数: 21

摘要

Glucosyl derivates exhibited favorable distribution to the brain. However, bidirectional transport of glucose transporter 1 might decrease concentrations of the prodrugs in brain before the release of parent drugs. To overcome this defect, glucosyl thiamine disulfide prodrugs 1a–1c incorporating naproxen were designed and synthesized. Furthermore, prodrug 2 and 3 were also prepared as control. The favorable physicochemical properties ...