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Page 1
Discovery of Indazoles as Potent, Orally Active Dual Neurokinin 1 Receptor Antagonists and Serotonin Transporter Inhibitors for the Treatment of Depression.
Degnan AP, Tora GO, Huang H, Conlon DA, Davis CD, Hanumegowda UM, Hou X, Hsiao Y, Hu J, Krause R, Li YW, Newton AE, Pieschl RL, Raybon J, Rosner T, Sun JH, Taber MT, Taylor SJ, Wong MK, Zhang H, Lodge NJ, Bronson JJ, Macor JE, Gillman KW. Degnan AP, et al. Among authors: tora go. ACS Chem Neurosci. 2016 Dec 21;7(12):1635-1640. doi: 10.1021/acschemneuro.6b00337. Epub 2016 Oct 18. ACS Chem Neurosci. 2016. PMID: 27744678
Design, optimization, and in vivo evaluation of a series of pyridine derivatives with dual NK1 antagonism and SERT inhibition for the treatment of depression.
Gillman KW, Parker MF, Silva M, Degnan AP, Tora GO, Lodge NJ, Li YW, Lelas S, Taber M, Krause RG, Bertekap RL, Newton AE, Pieschl RL, Lengyel KD, Johnson KA, Taylor SJ, Bronson JJ, Macor JE. Gillman KW, et al. Among authors: tora go. Bioorg Med Chem Lett. 2013 Jan 15;23(2):407-11. doi: 10.1016/j.bmcl.2012.11.094. Epub 2012 Nov 30. Bioorg Med Chem Lett. 2013. PMID: 23253443
Biaryls as potent, tunable dual neurokinin 1 receptor antagonists and serotonin transporter inhibitors.
Degnan AP, Tora GO, Han Y, Rajamani R, Bertekap R, Krause R, Davis CD, Hu J, Morgan D, Taylor SJ, Krause K, Li YW, Mattson G, Cunningham MA, Taber MT, Lodge NJ, Bronson JJ, Gillman KW, Macor JE. Degnan AP, et al. Among authors: tora go. Bioorg Med Chem Lett. 2015 Aug 1;25(15):3039-43. doi: 10.1016/j.bmcl.2015.04.098. Epub 2015 Jun 2. Bioorg Med Chem Lett. 2015. PMID: 26048800
The synthesis and SAR of calcitonin gene-related peptide (CGRP) receptor antagonists derived from tyrosine surrogates. Part 2.
Han X, Civiello RL, Conway CM, Cook DA, Davis CD, Degnan AP, Jiang XJ, Macci R, Mathias NR, Moench P, Pin SS, Schartman R, Signor LJ, Thalody G, Tora G, Whiterock V, Xu C, Macor JE, Dubowchik GM. Han X, et al. Bioorg Med Chem Lett. 2013 Mar 15;23(6):1870-3. doi: 10.1016/j.bmcl.2013.01.011. Epub 2013 Jan 24. Bioorg Med Chem Lett. 2013. PMID: 23402880
Sulfonylated Benzothiazoles as Inhibitors of Endothelial Lipase.
Johnson JA, Tora G, Pi Z, Phillips M, Yin X, Yang R, Zhao L, Chen AY, Taylor DS, Basso M, Rose A, Behnia K, Onorato J, Chen XQ, Abell LM, Lu H, Locke G, Caporuscio C, Galella M, Adam LP, Gordon D, Wexler RR, Finlay HJ. Johnson JA, et al. ACS Med Chem Lett. 2018 Nov 21;9(12):1263-1268. doi: 10.1021/acsmedchemlett.8b00424. eCollection 2018 Dec 13. ACS Med Chem Lett. 2018. PMID: 30613337 Free PMC article.
Identification of substituted benzothiazole sulfones as potent and selective inhibitors of endothelial lipase.
Kim SH, Johnson JA, Jiang J, Parkhurst B, Phillips M, Pi Z, Qiao JX, Tora G, Ye Chen A, Liu E, Yin X, Yang R, Zhao L, Taylor DS, Basso M, Behnia K, Onorato J, Chen XQ, Abell LM, Lu H, Locke G, Caporuscio C, Adam LP, Gordon D, Wexler RR, Finlay HJ. Kim SH, et al. Bioorg Med Chem Lett. 2019 Aug 1;29(15):1918-1921. doi: 10.1016/j.bmcl.2019.05.048. Epub 2019 May 25. Bioorg Med Chem Lett. 2019. PMID: 31176700
Corrigendum to "Identification of substituted benzothiazole sulfones as potent and selective inhibitors of endothelial lipase" [Bioorg. Med. Chem. Lett. 29 (2019) 1918-1921].
Kim SH, Johnson JA, Jiang J, Parkhurst B, Phillips M, Pi Z, Qiao JX, Tora G, Ye Chen A, Liu E, Yin X, Yang R, Zhao L, Taylor DS, Basso M, Behnia K, Onorato J, Chen XQ, Abell LM, Lu H, Locke G, Caporuscio C, Adam LP, Gordon D, Wexler RR, Finlay HJ. Kim SH, et al. Bioorg Med Chem Lett. 2019 Sep 1;29(17):2525. doi: 10.1016/j.bmcl.2019.07.032. Epub 2019 Jul 25. Bioorg Med Chem Lett. 2019. PMID: 31353296 No abstract available.
Identification of Reversible Small Molecule Inhibitors of Endothelial Lipase (EL) That Demonstrate HDL-C Increase In Vivo.
Tora G, Kim SH, Pi Z, Johnson JA, Jiang J, Phillips M, Lloyd J, Abell LM, Lu H, Locke G, Adam LP, Taylor DS, Yin X, Behnia K, Zhao L, Yang R, Basso M, Caporuscio C, Chen AY, Liu E, Kirshgessner T, Onorato JM, Ryan C, Traeger SC, Gordon D, Wexler RR, Finlay HJ. Tora G, et al. J Med Chem. 2020 Feb 27;63(4):1660-1670. doi: 10.1021/acs.jmedchem.9b01831. Epub 2020 Feb 11. J Med Chem. 2020. PMID: 31990537