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The discovery and optimization of benzimidazoles as selective NaV1.8 blockers for the treatment of pain.
Brown AD, Bagal SK, Blackwell P, Blakemore DC, Brown B, Bungay PJ, Corless M, Crawforth J, Fengas D, Fenwick DR, Gray V, Kemp M, Klute W, Malet Sanz L, Miller D, Murata Y, Payne CE, Skerratt S, Stevens EB, Warmus JS. Brown AD, et al. Among authors: bagal sk. Bioorg Med Chem. 2019 Jan 1;27(1):230-239. doi: 10.1016/j.bmc.2018.12.002. Epub 2018 Dec 4. Bioorg Med Chem. 2019. PMID: 30538065
Medicinal chemistry approaches to avoid aldehyde oxidase metabolism.
Pryde DC, Tran TD, Jones P, Duckworth J, Howard M, Gardner I, Hyland R, Webster R, Wenham T, Bagal S, Omoto K, Schneider RP, Lin J. Pryde DC, et al. Bioorg Med Chem Lett. 2012 Apr 15;22(8):2856-60. doi: 10.1016/j.bmcl.2012.02.069. Epub 2012 Mar 3. Bioorg Med Chem Lett. 2012. PMID: 22429467
Ion channels as therapeutic targets: a drug discovery perspective.
Bagal SK, Brown AD, Cox PJ, Omoto K, Owen RM, Pryde DC, Sidders B, Skerratt SE, Stevens EB, Storer RI, Swain NA. Bagal SK, et al. J Med Chem. 2013 Feb 14;56(3):593-624. doi: 10.1021/jm3011433. Epub 2012 Nov 29. J Med Chem. 2013. PMID: 23121096 Review.
Recent progress in sodium channel modulators for pain.
Bagal SK, Chapman ML, Marron BE, Prime R, Storer RI, Swain NA. Bagal SK, et al. Bioorg Med Chem Lett. 2014 Aug 15;24(16):3690-9. doi: 10.1016/j.bmcl.2014.06.038. Epub 2014 Jun 21. Bioorg Med Chem Lett. 2014. PMID: 25060923 Free article. Review.
A novel selective and orally bioavailable Nav 1.8 channel blocker, PF-01247324, attenuates nociception and sensory neuron excitability.
Payne CE, Brown AR, Theile JW, Loucif AJ, Alexandrou AJ, Fuller MD, Mahoney JH, Antonio BM, Gerlach AC, Printzenhoff DM, Prime RL, Stockbridge G, Kirkup AJ, Bannon AW, England S, Chapman ML, Bagal S, Roeloffs R, Anand U, Anand P, Bungay PJ, Kemp M, Butt RP, Stevens EB. Payne CE, et al. Br J Pharmacol. 2015 May;172(10):2654-70. doi: 10.1111/bph.13092. Epub 2015 Apr 10. Br J Pharmacol. 2015. PMID: 25625641 Free PMC article.
Discovery and Optimization of Selective Nav1.8 Modulator Series That Demonstrate Efficacy in Preclinical Models of Pain.
Bagal SK, Bungay PJ, Denton SM, Gibson KR, Glossop MS, Hay TL, Kemp MI, Lane CA, Lewis ML, Maw GN, Million WA, Payne CE, Poinsard C, Rawson DJ, Stammen BL, Stevens EB, Thompson LR. Bagal SK, et al. ACS Med Chem Lett. 2015 Apr 29;6(6):650-4. doi: 10.1021/acsmedchemlett.5b00059. eCollection 2015 Jun 11. ACS Med Chem Lett. 2015. PMID: 26101568 Free PMC article.
The Discovery of a Potent, Selective, and Peripherally Restricted Pan-Trk Inhibitor (PF-06273340) for the Treatment of Pain.
Skerratt SE, Andrews M, Bagal SK, Bilsland J, Brown D, Bungay PJ, Cole S, Gibson KR, Jones R, Morao I, Nedderman A, Omoto K, Robinson C, Ryckmans T, Skinner K, Stupple P, Waldron G. Skerratt SE, et al. Among authors: bagal sk. J Med Chem. 2016 Nov 23;59(22):10084-10099. doi: 10.1021/acs.jmedchem.6b00850. Epub 2016 Nov 4. J Med Chem. 2016. PMID: 27766865
29 results