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Synthesis, attempted kinetic resolution and evaluation of [123I]-MK-447 analogues as inflammation radiopharmaceuticals

Journal Article


Abstract


  • The non-steroidal anti-inflammatory agent 2-amino-methyl-4-tert-butyl-6-iodophenol hydrochloride (MK-447) and some of its analogues were labelled with 123I and tested in an inflamed rat-paw model. Even though MK-447 has a significant anti-inflammatory activity, and a 2.3 ratio for inflamed site over muscle, its usefullness for scintigraphic detection of inflammation is hindered by its high uptake in the skin. The kinetic resolution of diastereomeric products with chiral dienyl iron complexes was unsuccessful as the signals from the respective 1H and 13C NMR spectra were coincident.

Publication Date


  • 1997

Scopus Eid


  • 2-s2.0-0030792003

Web Of Science Accession Number


Start Page


  • 711

End Page


  • 729

Volume


  • 39

Issue


  • 9

Abstract


  • The non-steroidal anti-inflammatory agent 2-amino-methyl-4-tert-butyl-6-iodophenol hydrochloride (MK-447) and some of its analogues were labelled with 123I and tested in an inflamed rat-paw model. Even though MK-447 has a significant anti-inflammatory activity, and a 2.3 ratio for inflamed site over muscle, its usefullness for scintigraphic detection of inflammation is hindered by its high uptake in the skin. The kinetic resolution of diastereomeric products with chiral dienyl iron complexes was unsuccessful as the signals from the respective 1H and 13C NMR spectra were coincident.

Publication Date


  • 1997

Scopus Eid


  • 2-s2.0-0030792003

Web Of Science Accession Number


Start Page


  • 711

End Page


  • 729

Volume


  • 39

Issue


  • 9