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Discovery of non-zwitterionic aryl sulfonamides as Nav1.7 inhibitors with efficacy in preclinical behavioral models and translational measures of nociceptive neuron activation.
Wu YJ, Guernon J, McClure A, Luo G, Rajamani R, Ng A, Easton A, Newton A, Bourin C, Parker D, Mosure K, Barnaby O, Soars MG, Knox RJ, Matchett M, Pieschl R, Herrington J, Chen P, Sivarao DV, Bristow LJ, Meanwell NA, Bronson J, Olson R, Thompson LA, Dzierba C. Wu YJ, et al. Bioorg Med Chem. 2017 Oct 15;25(20):5490-5505. doi: 10.1016/j.bmc.2017.08.012. Epub 2017 Aug 9. Bioorg Med Chem. 2017. PMID: 28818462
Development of New Benzenesulfonamides As Potent and Selective Nav1.7 Inhibitors for the Treatment of Pain.
Wu YJ, Guernon J, Shi J, Ditta J, Robbins KJ, Rajamani R, Easton A, Newton A, Bourin C, Mosure K, Soars MG, Knox RJ, Matchett M, Pieschl RL, Post-Munson DJ, Wang S, Herrington J, Graef J, Newberry K, Bristow LJ, Meanwell NA, Olson R, Thompson LA, Dzierba C. Wu YJ, et al. Among authors: pieschl rl. J Med Chem. 2017 Mar 23;60(6):2513-2525. doi: 10.1021/acs.jmedchem.6b01918. Epub 2017 Mar 10. J Med Chem. 2017. PMID: 28234467
Effects of BMS-902483, an α7 nicotinic acetylcholine receptor partial agonist, on cognition and sensory gating in relation to receptor occupancy in rodents.
Pieschl RL, Miller R, Jones KM, Post-Munson DJ, Chen P, Newberry K, Benitex Y, Molski T, Morgan D, McDonald IM, Macor JE, Olson RE, Asaka Y, Digavalli S, Easton A, Herrington J, Westphal RS, Lodge NJ, Zaczek R, Bristow LJ, Li YW. Pieschl RL, et al. Eur J Pharmacol. 2017 Jul 15;807:1-11. doi: 10.1016/j.ejphar.2017.04.024. Epub 2017 Apr 22. Eur J Pharmacol. 2017. PMID: 28438647
Discovery of morpholine-based aryl sulfonamides as Nav1.7 inhibitors.
Wu YJ, Guernon J, McClure A, Venables B, Rajamani R, Robbins KJ, Knox RJ, Matchett M, Pieschl RL, Herrington J, Bristow LJ, Meanwell NA, Olson R, Thompson LA, Dzierba C. Wu YJ, et al. Among authors: pieschl rl. Bioorg Med Chem Lett. 2018 Mar 1;28(5):958-962. doi: 10.1016/j.bmcl.2018.01.035. Epub 2018 Feb 1. Bioorg Med Chem Lett. 2018. PMID: 29439904
Discovery of Indole- and Indazole-acylsulfonamides as Potent and Selective NaV1.7 Inhibitors for the Treatment of Pain.
Luo G, Chen L, Easton A, Newton A, Bourin C, Shields E, Mosure K, Soars MG, Knox RJ, Matchett M, Pieschl RL, Post-Munson DJ, Wang S, Herrington J, Graef J, Newberry K, Sivarao DV, Senapati A, Bristow LJ, Meanwell NA, Thompson LA, Dzierba C. Luo G, et al. Among authors: pieschl rl. J Med Chem. 2019 Jan 24;62(2):831-856. doi: 10.1021/acs.jmedchem.8b01550. Epub 2019 Jan 8. J Med Chem. 2019. PMID: 30576602
Discovery of new indole-based acylsulfonamide Nav1.7 inhibitors.
Wu YJ, Venables B, Guernon J, Chen J, Sit SY, Rajamani R, Knox RJ, Matchett M, Pieschl RL, Herrington J, Bristow LJ, Meanwell NA, Thompson LA, Dzierba C. Wu YJ, et al. Among authors: pieschl rl. Bioorg Med Chem Lett. 2019 Feb 15;29(4):659-663. doi: 10.1016/j.bmcl.2018.12.013. Epub 2018 Dec 6. Bioorg Med Chem Lett. 2019. PMID: 30638874
The Novel, Nicotinic Alpha7 Receptor Partial Agonist, BMS-933043, Improves Cognition and Sensory Processing in Preclinical Models of Schizophrenia.
Bristow LJ, Easton AE, Li YW, Sivarao DV, Lidge R, Jones KM, Post-Munson D, Daly C, Lodge NJ, Gallagher L, Molski T, Pieschl R, Chen P, Hendricson A, Westphal R, Cook J, Iwuagwu C, Morgan D, Benitex Y, King D, Macor JE, Zaczek R, Olson R. Bristow LJ, et al. PLoS One. 2016 Jul 28;11(7):e0159996. doi: 10.1371/journal.pone.0159996. eCollection 2016. PLoS One. 2016. PMID: 27467081 Free PMC article.
41 results