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The Discovery and Hit-to-Lead Optimization of Tricyclic Sulfonamides as Potent and Efficacious Potentiators of Glycine Receptors.
Bregman H, Simard JR, Andrews KL, Ayube S, Chen H, Gunaydin H, Guzman-Perez A, Hu J, Huang L, Huang X, Krolikowski PH, Lehto SG, Lewis RT, Michelsen K, Pegman P, Plant MH, Shaffer PL, Teffera Y, Yi S, Zhang M, Gingras J, DiMauro EF. Bregman H, et al. J Med Chem. 2017 Feb 9;60(3):1105-1125. doi: 10.1021/acs.jmedchem.6b01496. Epub 2016 Dec 21. J Med Chem. 2017. PMID: 28001399
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: bregman h. 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
Crystal structures of human glycine receptor α3 bound to a novel class of analgesic potentiators.
Huang X, Shaffer PL, Ayube S, Bregman H, Chen H, Lehto SG, Luther JA, Matson DJ, McDonough SI, Michelsen K, Plant MH, Schneider S, Simard JR, Teffera Y, Yi S, Zhang M, DiMauro EF, Gingras J. Huang X, et al. Among authors: bregman h. Nat Struct Mol Biol. 2017 Feb;24(2):108-113. doi: 10.1038/nsmb.3329. Epub 2016 Dec 19. Nat Struct Mol Biol. 2017. PMID: 27991902
Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency and Pharmacokinetics While Mitigating Metabolic Liabilities.
Weiss MM, Dineen TA, Marx IE, Altmann S, Boezio A, Bregman H, Chu-Moyer M, DiMauro EF, Feric Bojic E, Foti RS, Gao H, Graceffa R, Gunaydin H, Guzman-Perez A, Huang H, Huang L, Jarosh M, Kornecook T, Kreiman CR, Ligutti J, La DS, Lin MJ, Liu D, Moyer BD, Nguyen HN, Peterson EA, Rose PE, Taborn K, Youngblood BD, Yu V, Fremeau RT Jr. Weiss MM, et al. Among authors: bregman h. J Med Chem. 2017 Jul 27;60(14):5969-5989. doi: 10.1021/acs.jmedchem.6b01851. Epub 2017 Apr 20. J Med Chem. 2017. PMID: 28287723
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. 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 of novel, induced-pocket binding oxazolidinones as potent, selective, and orally bioavailable tankyrase inhibitors.
Bregman H, Chakka N, Guzman-Perez A, Gunaydin H, Gu Y, Huang X, Berry V, Liu J, Teffera Y, Huang L, Egge B, Mullady EL, Schneider S, Andrews PS, Mishra A, Newcomb J, Serafino R, Strathdee CA, Turci SM, Wilson C, DiMauro EF. Bregman H, et al. J Med Chem. 2013 Jun 13;56(11):4320-42. doi: 10.1021/jm4000038. Epub 2013 May 23. J Med Chem. 2013. PMID: 23701517
52 results