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Page 1
Discovery of a novel series of quinolone α7 nicotinic acetylcholine receptor agonists.
McDonald IM, Mate RA, Zusi FC, Huang H, Post-Munson DJ, Ferrante MA, Gallagher L, Bertekap RL Jr, Knox RJ, Robertson BJ, Harden DG, Morgan DG, Lodge NJ, Dworetzky SI, Olson RE, Macor JE. McDonald IM, et al. Bioorg Med Chem Lett. 2013 Mar 15;23(6):1684-8. doi: 10.1016/j.bmcl.2013.01.070. Epub 2013 Jan 29. Bioorg Med Chem Lett. 2013. PMID: 23414838
Design and synthesis of a novel series of 4-heteroarylamino-1'-azaspiro[oxazole-5,3'-bicyclo[2.2.2]octanes as α7 nicotinic receptor agonists 2. Development of 4-heteroaryl SAR.
Iwuagwu C, King D, McDonald IM, Cook J, Zusi FC, Hill MD, Mate RA, Fang H, Knox R, Gallagher L, Post-Munson Amy Easton D, Miller R, Benitex Y, Siuciak J, Lodge N, Zaczek R, Morgan D, Bristow L, Macor JE, Olson RE. Iwuagwu C, et al. Among authors: knox r. Bioorg Med Chem Lett. 2017 Mar 1;27(5):1261-1266. doi: 10.1016/j.bmcl.2017.01.058. Epub 2017 Jan 20. Bioorg Med Chem Lett. 2017. PMID: 28169167
(S)-N-[1-(3-morpholin-4-ylphenyl)ethyl]- 3-phenylacrylamide: an orally bioavailable KCNQ2 opener with significant activity in a cortical spreading depression model of migraine.
Wu YJ, Boissard CG, Greco C, Gribkoff VK, Harden DG, He H, L'Heureux A, Kang SH, Kinney GG, Knox RJ, Natale J, Newton AE, Lehtinen-Oboma S, Sinz MW, Sivarao DV, Starrett JE Jr, Sun LQ, Tertyshnikova S, Thompson MW, Weaver D, Wong HS, Zhang L, Dworetzky SI. Wu YJ, et al. J Med Chem. 2003 Jul 17;46(15):3197-200. doi: 10.1021/jm034073f. J Med Chem. 2003. PMID: 12852750
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 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. Wu YJ, et al. J Med Chem. 2003 Aug 28;46(18):3778-81. doi: 10.1021/jm034111v. J Med Chem. 2003. PMID: 12930139
(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. 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. 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
663 results