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Page 1
Design of Conformationally Constrained Acyl Sulfonamide Isosteres: Identification of N-([1,2,4]Triazolo[4,3- a]pyridin-3-yl)methane-sulfonamides as Potent and Selective hNaV1.7 Inhibitors for the Treatment of Pain.
Focken T, Chowdhury S, Zenova A, Grimwood ME, Chabot C, Sheng T, Hemeon I, Decker SM, Wilson M, Bichler P, Jia Q, Sun S, Young C, Lin S, Goodchild SJ, Shuart NG, Chang E, Xie Z, Li B, Khakh K, Bankar G, Waldbrook M, Kwan R, Nelkenbrecher K, Karimi Tari P, Chahal N, Sojo L, Robinette CL, White AD, Chen CA, Zhang Y, Pang J, Chang JH, Hackos DH, Johnson JP Jr, Cohen CJ, Ortwine DF, Sutherlin DP, Dehnhardt CM, Safina BS. Focken T, et al. Among authors: bichler p. J Med Chem. 2018 Jun 14;61(11):4810-4831. doi: 10.1021/acs.jmedchem.7b01826. Epub 2018 May 23. J Med Chem. 2018. PMID: 29737846
Discovery of Aryl Sulfonamides as Isoform-Selective Inhibitors of NaV1.7 with Efficacy in Rodent Pain Models.
Focken T, Liu S, Chahal N, Dauphinais M, Grimwood ME, Chowdhury S, Hemeon I, Bichler P, Bogucki D, Waldbrook M, Bankar G, Sojo LE, Young C, Lin S, Shuart N, Kwan R, Pang J, Chang JH, Safina BS, Sutherlin DP, Johnson JP Jr, Dehnhardt CM, Mansour TS, Oballa RM, Cohen CJ, Robinette CL. Focken T, et al. Among authors: bichler p. ACS Med Chem Lett. 2016 Jan 19;7(3):277-82. doi: 10.1021/acsmedchemlett.5b00447. eCollection 2016 Mar 10. ACS Med Chem Lett. 2016. PMID: 26985315 Free PMC article.
Identification of aryl sulfonamides as novel and potent inhibitors of NaV1.5.
Sun S, Jia Q, Zenova AY, Lin S, Hussainkhel A, Mezeyova J, Chang E, Goodchild SJ, Xie Z, Lindgren A, de Boer G, Kwan R, Khakh K, Sojo L, Bichler P, Johnson JP Jr, Empfield JR, Cohen CJ, Dehnhardt CM, Dean R. Sun S, et al. Among authors: bichler p. Bioorg Med Chem Lett. 2021 Aug 1;45:128133. doi: 10.1016/j.bmcl.2021.128133. Epub 2021 May 24. Bioorg Med Chem Lett. 2021. PMID: 34044121
Discovery of novel cyclopentane carboxylic acids as potent and selective inhibitors of NaV1.7.
Sun S, Chowdhury S, Hemeon I, Hasan A, Wilson MS, Bergeron P, Jia Q, Zenova AY, Grimwood ME, Gong W, Decker SM, Bichler P, Andrez JC, Focken T, Ngyuen T, Zhu J, White AD, Bankar G, Howard S, Chang E, Khakh K, Lin S, Dean R, Johnson JP Jr, Chang JH, Hackos DH, McKerrall SJ, Sellers B, Ortwine DF, Cohen CJ, Safina BS, Sutherlin DP, Dehnhardt CM. Sun S, et al. Among authors: bichler p. Bioorg Med Chem Lett. 2025 Feb 1;116:130033. doi: 10.1016/j.bmcl.2024.130033. Epub 2024 Nov 22. Bioorg Med Chem Lett. 2025. PMID: 39580005