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

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Wu, Y.J. et al.

Wu, Davis, Dworetzky, Fitzpatrick, Harden, He, Knox, Newton, Philip, Polson, Sivarao, Sun, Tertyshnikova, Weaver, Yeola, Zoeckler, Sinz,

Fluorine substitution can block CYP3A4 metabolism-dependent inhibition: identification of (S)-N-[1-(4-fluoro-3- morpholin-4-ylphenyl)ethyl]-3- (4-fluorophenyl)acrylamide as an orally bioavailable KCNQ2 opener devoid of CYP3A4 metabolism-dependent inhibition.

The formation of a reactive intermediate was found to be responsible for CYP3A4 metabolism-dependent inhibition (MDI) observed with (S)-N-[1-(3-morpholin-4-ylphenyl)ethyl]-3-phenyl-acrylamide (1). Structure-3A4 MDI relationship studies culminated in the discovery of a difluoro analogue, (S)-N-[1-(4-fluoro-3-morpholin-4-ylphenyl)ethyl]-3-(4-fluoro-phenyl)acrylamide (2), as an orally bioavailable KCNQ2 opener free of CYP3A4 MDI.[1]

References

Fluorine substitution can block CYP3A4 metabolism-dependent inhibition: identification of (S)-N-[1-(4-fluoro-3- morpholin-4-ylphenyl)ethyl]-3- (4-fluorophenyl)acrylamide as an orally bioavailable KCNQ2 opener devoid of CYP3A4 metabolism-dependent inhibition. Wu, Y.J., Davis, C.D., Dworetzky, S., Fitzpatrick, W.C., Harden, D., He, H., Knox, R.J., Newton, A.E., Philip, T., Polson, C., Sivarao, D.V., Sun, L.Q., Tertyshnikova, S., Weaver, D., Yeola, S., Zoeckler, M., Sinz, M.W. J. Med. Chem. (2003) [Pubmed]

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