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Page 1
The discovery of benzoxazine sulfonamide inhibitors of NaV1.7: Tools that bridge efficacy and target engagement.
La DS, Peterson EA, Bode C, Boezio AA, Bregman H, Chu-Moyer MY, Coats J, DiMauro EF, Dineen TA, Du B, Gao H, Graceffa R, Gunaydin H, Guzman-Perez A, Fremeau R Jr, Huang X, Ilch C, Kornecook TJ, Kreiman C, Ligutti J, Jasmine Lin MH, McDermott JS, Marx I, Matson DJ, McDonough SI, Moyer BD, Nho Nguyen H, Taborn K, Yu V, Weiss MM. La DS, et al. Among authors: ligutti j. Bioorg Med Chem Lett. 2017 Aug 1;27(15):3477-3485. doi: 10.1016/j.bmcl.2017.05.070. Epub 2017 Jun 1. Bioorg Med Chem Lett. 2017. PMID: 28629594
Identification of a potent, state-dependent inhibitor of Nav1.7 with oral efficacy in the formalin model of persistent pain.
Bregman H, Berry L, Buchanan JL, Chen A, Du B, Feric E, Hierl M, Huang L, Immke D, Janosky B, Johnson D, Li X, Ligutti J, Liu D, Malmberg A, Matson D, McDermott J, Miu P, Nguyen HN, Patel VF, Waldon D, Wilenkin B, Zheng XM, Zou A, McDonough SI, DiMauro EF. Bregman H, et al. Among authors: ligutti j. J Med Chem. 2011 Jul 14;54(13):4427-45. doi: 10.1021/jm200018k. Epub 2011 Jun 2. J Med Chem. 2011. PMID: 21634377
Discovery and optimization of aminopyrimidinones as potent and state-dependent Nav1.7 antagonists.
Nguyen HN, Bregman H, Buchanan JL, Du B, Feric E, Huang L, Li X, Ligutti J, Liu D, Malmberg AB, Matson DJ, McDermott JS, Patel VF, Wilenkin B, Zou A, McDonough SI, Dimauro EF. Nguyen HN, et al. Among authors: ligutti j. Bioorg Med Chem Lett. 2012 Jan 15;22(2):1055-60. doi: 10.1016/j.bmcl.2011.11.111. Epub 2011 Dec 6. Bioorg Med Chem Lett. 2012. PMID: 22209205
Application of a Parallel Synthetic Strategy in the Discovery of Biaryl Acyl Sulfonamides as Efficient and Selective NaV1.7 Inhibitors.
DiMauro EF, Altmann S, Berry LM, Bregman H, Chakka N, Chu-Moyer M, Bojic EF, Foti RS, Fremeau R, Gao H, Gunaydin H, Guzman-Perez A, Hall BE, Huang H, Jarosh M, Kornecook T, Lee J, Ligutti J, Liu D, Moyer BD, Ortuno D, Rose PE, Schenkel LB, Taborn K, Wang J, Wang Y, Yu V, Weiss MM. DiMauro EF, et al. Among authors: ligutti j. J Med Chem. 2016 Sep 8;59(17):7818-39. doi: 10.1021/acs.jmedchem.6b00425. Epub 2016 Aug 29. J Med Chem. 2016. PMID: 27441383
Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency and Pharmacokinetics to Enable in Vivo Target Engagement.
Marx IE, Dineen TA, Able J, Bode C, Bregman H, Chu-Moyer M, DiMauro EF, Du B, Foti RS, Fremeau RT Jr, Gao H, Gunaydin H, Hall BE, Huang L, Kornecook T, Kreiman CR, La DS, Ligutti J, Lin MJ, Liu D, McDermott JS, Moyer BD, Peterson EA, Roberts JT, Rose P, Wang J, Youngblood BD, Yu V, Weiss MM. Marx IE, et al. Among authors: ligutti j. ACS Med Chem Lett. 2016 Sep 21;7(12):1062-1067. doi: 10.1021/acsmedchemlett.6b00243. eCollection 2016 Dec 8. ACS Med Chem Lett. 2016. PMID: 27994738 Free PMC article.
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