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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. [electronic resource] by
- Wu, Yong-Jin
- Davis, Carl D
- Dworetzky, Steven
- Fitzpatrick, William C
- Harden, David
- He, Huan
- Knox, Ronald J
- Newton, Amy E
- Philip, Thomas
- Polson, Craig
- Sivarao, Digavalli V
- Sun, Li-Qiang
- Tertyshnikova, Svetlana
- Weaver, David
- Yeola, Suresh
- Zoeckler, Mary
- Sinz, Michael W
Producer: 20030916
In:
Journal of medicinal chemistry vol. 46
Availability: No items available.
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(S)-N-[1-(4-cyclopropylmethyl-3,4-dihydro-2H-benzo[1,4]oxazin-6-yl)-ethyl]-3-(2-fluoro-phenyl)-acrylamide is a potent and efficacious KCNQ2 opener which inhibits induced hyperexcitability of rat hippocampal neurons. [electronic resource] by
- Wu, Yong-Jin
- Boissard, Christopher G
- Chen, Jie
- Fitzpatrick, William
- Gao, Qi
- Gribkoff, Valentin K
- Harden, David G
- He, Huan
- Knox, Ronald J
- Natale, Joanne
- Pieschl, Rick L
- Starrett, John E
- Sun, Li-Qiang
- Thompson, Mark
- Weaver, David
- Wu, Dedong
- Dworetzky, Steven I
Producer: 20041109
In:
Bioorganic & medicinal chemistry letters vol. 14
Availability: No items available.
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8.
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Synthesis and KCNQ2 opener activity of N-(1-benzo[1,3]dioxol-5-yl-ethyl, N-[1-(2,3-dihydro-benzofuran-5-yl)-ethyl, and N-[1-(2,3-dihydro-1H-indol-5-yl)-ethyl acrylamides. [electronic resource] by
- Wu, Yong-Jin
- Sun, Li-Qiang
- He, Huan
- Chen, Jie
- Starrett, John E
- Dextraze, Pierre
- Daris, Jean-Paul
- Boissard, Christopher G
- Pieschl, Rick L
- Gribkoff, Valentin K
- Natale, Joanne
- Knox, Ronald J
- Harden, David G
- Thompson, Mark W
- Fitzpatrick, William
- Weaver, David
- Wu, Dedong
- Gao, Qi
- Dworetzky, Steven I
Producer: 20050209
In:
Bioorganic & medicinal chemistry letters vol. 14
Availability: No items available.
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Discovery of (S,E)-3-(2-fluorophenyl)-N-(1-(3-(pyridin-3-yloxy)phenyl)ethyl)-acrylamide as a potent and efficacious KCNQ2 (Kv7.2) opener for the treatment of neuropathic pain. [electronic resource] by
- Wu, Yong-Jin
- Conway, Charles M
- Sun, Li-Qiang
- Machet, Frederic
- Chen, Jie
- Chen, Ping
- He, Huan
- Bourin, Clotilde
- Calandra, Vincenzo
- Polino, Joseph L
- Davis, Carl D
- Heman, Karen
- Gribkoff, Valentin K
- Boissard, Christopher G
- Knox, Ronald J
- Thompson, Mark W
- Fitzpatrick, William
- Weaver, David
- Harden, David G
- Natale, Joanne
- Dworetzky, Steven I
- Starrett, John E
Producer: 20140722
In:
Bioorganic & medicinal chemistry letters vol. 23
Availability: No items available.
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