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

Yong Jin Wu; Carl D. Davis; Steven Dworetzky; William C. Fitzpatrick; David Harden; Huan He; Ronald J. Knox; Amy E. Newton; Thomas Philip; Craig Polson; Digavalli V. Sivarao; Li Qiang Sun; Svetlana Tertyshnikova; David Weaver; Suresh Yeola; Mary Zoeckler; Michael W. Sinz

doi:10.1021/jm034111v

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

Yong Jin Wu
, Carl D. Davis
, Steven Dworetzky
, William C. Fitzpatrick
, David Harden
, Huan He
, Ronald J. Knox
, Amy E. Newton
, Thomas Philip
, Craig Polson
, Digavalli V. Sivarao
, Li Qiang Sun
, Svetlana Tertyshnikova
, David Weaver
, Suresh Yeola
, Mary Zoeckler
, Michael W. Sinz

Department of Pharmaceutical Sciences

Bristol-Myers Squibb

Research output: Contribution to journal › Article › peer-review

Original language	English
Pages (from-to)	3778-3781
Number of pages	4
Journal	Journal of Medicinal Chemistry
Volume	46
Issue number	18
DOIs	https://doi.org/10.1021/jm034111v
State	Published - Aug 2003

ASJC Scopus Subject Areas

Molecular Medicine
Drug Discovery

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10.1021/jm034111v

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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. (2003). 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. Journal of Medicinal Chemistry, 46(18), 3778-3781. https://doi.org/10.1021/jm034111v

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, Yong Jin; Davis, Carl D.; Dworetzky, Steven et al.
In: Journal of Medicinal Chemistry, Vol. 46, No. 18, 08.2003, p. 3778-3781.

Research output: Contribution to journal › Article › peer-review

Wu, YJ, Davis, CD, Dworetzky, S, Fitzpatrick, WC, Harden, D, He, H, Knox, RJ, Newton, AE, Philip, T, Polson, C, Sivarao, DV, Sun, LQ, Tertyshnikova, S, Weaver, D, Yeola, S, Zoeckler, M & Sinz, MW 2003, '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', Journal of Medicinal Chemistry, vol. 46, no. 18, pp. 3778-3781. https://doi.org/10.1021/jm034111v

Wu YJ, Davis CD, Dworetzky S, Fitzpatrick WC, Harden D, He H et al. 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. Journal of Medicinal Chemistry. 2003 Aug;46(18):3778-3781. doi: 10.1021/jm034111v

Wu, Yong Jin ; Davis, Carl D. ; Dworetzky, Steven et al. / 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. In: Journal of Medicinal Chemistry. 2003 ; Vol. 46, No. 18. pp. 3778-3781.

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title = "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",

author = "Wu, \{Yong Jin\} and Davis, \{Carl D.\} and Steven Dworetzky and Fitzpatrick, \{William C.\} and David Harden and Huan He and Knox, \{Ronald J.\} and Newton, \{Amy E.\} and Thomas Philip and Craig Polson and Sivarao, \{Digavalli V.\} and Sun, \{Li Qiang\} and Svetlana Tertyshnikova and David Weaver and Suresh Yeola and Mary Zoeckler and Sinz, \{Michael W.\}",

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AU - Wu, Yong Jin

AU - Davis, Carl D.

AU - Dworetzky, Steven

AU - Fitzpatrick, William C.

AU - Harden, David

AU - He, Huan

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AU - Philip, Thomas

AU - Polson, Craig

AU - Sivarao, Digavalli V.

AU - Sun, Li Qiang

AU - Tertyshnikova, Svetlana

AU - Weaver, David

AU - Yeola, Suresh

AU - Zoeckler, Mary

AU - Sinz, Michael W.

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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

ASJC Scopus Subject Areas

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