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

Evaluation of hydroxyimine as cytochrome P450-selective prodrug structure.

Hydroxyimine derivatives of ketoprofen (1) and nabumetone (2) were synthesized and evaluated in vitro and in vivo as cytochrome P450-selective intermediate prodrug structures of ketones. 2 released nabumetone in vitro in the presence of isolated rat and human liver microsomes and in different recombinant human CYP isoforms. Bioconversion of 2 to both nabumetone and its active metabolite, 6-methoxy-2-naphthylacetic acid (6-MNA), was further confirmed in rats in vivo. Results indicate that hydroxyimine is a useful intermediate prodrug structure for ketone drugs.[1]

References

  1. Evaluation of hydroxyimine as cytochrome P450-selective prodrug structure. Kumpulainen, H., Mähönen, N., Laitinen, M.L., Jaurakkajärvi, M., Raunio, H., Juvonen, R.O., Vepsäläinen, J., Järvinen, T., Rautio, J. J. Med. Chem. (2006) [Pubmed]
 
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