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  • Title: Evaluation of hydroxyimine as cytochrome P450-selective prodrug structure.
    Author: Kumpulainen H, Mähönen N, Laitinen ML, Jaurakkajärvi M, Raunio H, Juvonen RO, Vepsäläinen J, Järvinen T, Rautio J.
    Journal: J Med Chem; 2006 Feb 09; 49(3):1207-11. PubMed ID: 16451086.
    Abstract:
    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.
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