| Literature DB >> 16451086 |
Hanna Kumpulainen1, Niina Mähönen, Marja-Leena Laitinen, Marja Jaurakkajärvi, Hannu Raunio, Risto O Juvonen, Jouko Vepsäläinen, Tomi Järvinen, Jarkko Rautio.
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.Entities:
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Year: 2006 PMID： 16451086 DOI： 10.1021/jm0510124
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446