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Identification of a potent and selective 5-HT(6) antagonist: one-step synthesis of (E)-3-(benzenesulfonyl)-2- (methylsulfanyl)pyrido[1,2-a]pyrimidin-4-ylidenamine from 2-(benzenesulfonyl)-3,3-bis(methylsulfanyl)acrylonitrile.
Wu YJ, He H, Hu S, Huang Y, Scola PM, Grant-Young K, Bertekap RL, Wu D, Gao Q, Li Y, Klakouski C, Westphal RS. Wu YJ, et al. Among authors: wu d. J Med Chem. 2003 Nov 6;46(23):4834-7. doi: 10.1021/jm034142q. J Med Chem. 2003. PMID: 14584934
(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.
Wu YJ, Boissard CG, Chen J, Fitzpatrick W, Gao Q, Gribkoff VK, Harden DG, He H, Knox RJ, Natale J, Pieschl RL, Starrett JE Jr, Sun LQ, Thompson M, Weaver D, Wu D, Dworetzky SI. Wu YJ, et al. Among authors: wu d. Bioorg Med Chem Lett. 2004 Apr 19;14(8):1991-5. doi: 10.1016/j.bmcl.2004.01.069. Bioorg Med Chem Lett. 2004. PMID: 15050644
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.
Wu YJ, Sun LQ, He H, Chen J, Starrett JE Jr, Dextraze P, Daris JP, Boissard CG, Pieschl RL, Gribkoff VK, Natale J, Knox RJ, Harden DG, Thompson MW, Fitzpatrick W, Weaver D, Wu D, Gao Q, Dworetzky SI. Wu YJ, et al. Among authors: wu d. Bioorg Med Chem Lett. 2004 Sep 6;14(17):4533-7. doi: 10.1016/j.bmcl.2004.06.035. Bioorg Med Chem Lett. 2004. PMID: 15357987
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.
Wu YJ, Conway CM, Sun LQ, Machet F, Chen J, Chen P, He H, Bourin C, Calandra V, Polino JL, Davis CD, Heman K, Gribkoff VK, Boissard CG, Knox RJ, Thompson MW, Fitzpatrick W, Weaver D, Harden DG, Natale J, Dworetzky SI, Starrett JE Jr. Wu YJ, et al. Bioorg Med Chem Lett. 2013 Nov 15;23(22):6188-91. doi: 10.1016/j.bmcl.2013.08.092. Epub 2013 Sep 8. Bioorg Med Chem Lett. 2013. PMID: 24070783
1,915 results