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  • Title: Design, synthesis and biological evaluation of brain-specific glucosyl thiamine disulfide prodrugs of naproxen.
    Author: Fan W, Wu Y, Li XK, Yao N, Li X, Yu YG, Hai L.
    Journal: Eur J Med Chem; 2011 Sep; 46(9):3651-61. PubMed ID: 21641697.
    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 of these prodrugs were verified by stability and metabolism studies. Results from the in vivo distribution study indicated that 1a-1c, and 1b in particular, significantly increased the level of naproxen in brain when compared to 2 and 3. The study suggested glucosyl thiamine disulfide was a promising carrier to enhance the brain bioavailability of central nervous system active drugs.
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