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2-[(3aR,4R,5S,7aS)-5-{(1S)-1-[3,5-bis(trifluoromethyl)phenyl]-2-hydroxyethoxy}-4-(2-methylphenyl)octahydro-2H-isoindol-2-yl]-1,3-oxazol-4(5H)-one: a potent human NK1 receptor antagonist with multiple clearance pathways.
Kassick AJ, Jiang J, Bunda J, Wilson D, Bao J, Lu H, Lin P, Ball RG, Doss GA, Tong X, Tsao KL, Wang H, Chicchi G, Karanam B, Tschirret-Guth R, Samuel K, Hora DF, Kumar S, Madeira M, Eng W, Hargreaves R, Purcell M, Gantert L, Cook J, DeVita RJ, Mills SG. Kassick AJ, et al. Among authors: tsao kl. J Med Chem. 2013 Jul 25;56(14):5940-8. doi: 10.1021/jm400751p. Epub 2013 Jul 9. J Med Chem. 2013. PMID: 23808489
The discovery of potent, selective, and orally bioavailable hNK1 antagonists derived from pyrrolidine.
Lin P, Chang L, Devita RJ, Young JR, Eid R, Tong X, Zheng S, Ball RG, Tsou NN, Chicchi GG, Kurtz MM, Tsao KL, Wheeldon A, Carlson EJ, Eng W, Burns HD, Hargreaves RJ, Mills SG. Lin P, et al. Among authors: tsao kl. Bioorg Med Chem Lett. 2007 Sep 15;17(18):5191-8. doi: 10.1016/j.bmcl.2007.06.085. Epub 2007 Jul 4. Bioorg Med Chem Lett. 2007. PMID: 17637506
Fused bicyclic pyrrolizinones as new scaffolds for human NK1 antagonists.
Morriello GJ, Devita RJ, Mills SG, Young JR, Lin P, Doss G, Chicchi GG, Demartino J, Kurtz MM, Tsao KL, Carlson E, Townson K, Wheeldon A, Boyce S, Collinson N, Rupniak N, Moore S. Morriello GJ, et al. Among authors: tsao kl. Bioorg Med Chem. 2008 Mar 1;16(5):2156-70. doi: 10.1016/j.bmc.2007.11.081. Epub 2007 Dec 5. Bioorg Med Chem. 2008. PMID: 18248994
Potent, brain-penetrant, hydroisoindoline-based human neurokinin-1 receptor antagonists.
Jiang J, Bunda JL, Doss GA, Chicchi GG, Kurtz MM, Tsao KL, Tong X, Zheng S, Upthagrove A, Samuel K, Tschirret-Guth R, Kumar S, Wheeldon A, Carlson EJ, Hargreaves R, Burns D, Hamill T, Ryan C, Krause SM, Eng W, DeVita RJ, Mills SG. Jiang J, et al. Among authors: tsao kl. J Med Chem. 2009 May 14;52(9):3039-46. doi: 10.1021/jm8016514. J Med Chem. 2009. PMID: 19354254
Tetrahydroindolizinone NK1 antagonists.
Bao J, Lu H, Morriello GJ, Carlson EJ, Wheeldon A, Chicchi GG, Kurtz MM, Tsao KL, Zheng S, Tong X, Mills SG, DeVita RJ. Bao J, et al. Among authors: tsao kl. Bioorg Med Chem Lett. 2010 Apr 1;20(7):2354-8. doi: 10.1016/j.bmcl.2010.01.120. Epub 2010 Feb 1. Bioorg Med Chem Lett. 2010. PMID: 20188553
Pyrrolidine-carboxamides and oxadiazoles as potent hNK1 antagonists.
Young JR, Eid R, Turner C, DeVita RJ, Kurtz MM, Tsao KL, Chicchi GG, Wheeldon A, Carlson E, Mills SG. Young JR, et al. Among authors: tsao kl. Bioorg Med Chem Lett. 2007 Oct 1;17(19):5310-5. doi: 10.1016/j.bmcl.2007.08.028. Epub 2007 Aug 16. Bioorg Med Chem Lett. 2007. PMID: 17723300
Discovery and Pharmacology of a Novel Somatostatin Subtype 5 (SSTR5) Antagonist: Synergy with DPP-4 Inhibition.
Liu W, Shao PP, Liang GB, Bawiec J, He J, Aster SD, Wu M, Chicchi G, Wang J, Tsao KL, Shang J, Salituro G, Zhou YP, Li C, Akiyama TE, Metzger DE, Murphy BA, Howard AD, Weber AE, Duffy JL. Liu W, et al. Among authors: tsao kl. ACS Med Chem Lett. 2018 Sep 12;9(11):1082-1087. doi: 10.1021/acsmedchemlett.8b00305. eCollection 2018 Nov 8. ACS Med Chem Lett. 2018. PMID: 30429949 Free PMC article.
SAR exploration at the C-3 position of tetrahydro-β-carboline sstr3 antagonists.
He S, Dobbelaar PH, Guo L, Ye Z, Liu J, Jian T, Truong Q, Shah SK, Du W, Qi H, Bakshi RK, Hong Q, Dellureficio JD, Sherer E, Pasternak A, Feng Z, Reibarkh M, Lin M, Samuel K, Reddy VB, Mitelman S, Tong SX, Chicchi GG, Tsao KL, Trusca D, Wu M, Shao Q, Trujillo ME, Fernandez G, Nelson D, Bunting P, Kerr J, Fitzgerald P, Morissette P, Volksdorf S, Eiermann GJ, Li C, Zhang BB, Howard AD, Zhou YP, Nargund RP, Hagmann WK. He S, et al. Among authors: tsao kl. Bioorg Med Chem Lett. 2016 Mar 15;26(6):1529-1535. doi: 10.1016/j.bmcl.2016.02.022. Epub 2016 Feb 10. Bioorg Med Chem Lett. 2016. PMID: 26898814
39 results