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…

Index: 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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Citation Number: 21

Abstract

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 ...