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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 
 
 

Design and synthesis of a novel L-dopa-entacapone codrug.

A novel codrug, in which L-Dopa and entacapone are linked via a biodegradable carbamate spacer to form a single chemical entity, was synthesized and studied kinetically. This carbamate codrug provides adequate stability [t(1/2) = 12.1 h (pH 1.2); 1.4 h (pH 5.0); 1.1 h (pH 7.4)] against chemical hydrolysis but rapidly hydrolyzes to L-Dopa and entacapone in liver homogenate (t(1/2) = 7 min; pH 7.4) at 37 degrees C. The therapeutical potential of this novel codrug is discussed.[1]

References

  1. Design and synthesis of a novel L-dopa-entacapone codrug. Leppänen, J., Huuskonen, J., Nevalainen, T., Gynther, J., Taipale, H., Järvinen, T. J. Med. Chem. (2002) [Pubmed]
 
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