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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: bao j. J Med Chem. 2013 Jul 25;56(14):5940-8. doi: 10.1021/jm400751p. Epub 2013 Jul 9. J Med Chem. 2013. PMID: 23808489
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. 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
Discovery of [11C]MK-6884: A Positron Emission Tomography (PET) Imaging Agent for the Study of M4Muscarinic Receptor Positive Allosteric Modulators (PAMs) in Neurodegenerative Diseases.
Tong L, Li W, Lo MM, Gao X, Wai JM, Rudd M, Tellers D, Joshi A, Zeng Z, Miller P, Salinas C, Riffel K, Haley H, Purcell M, Holahan M, Gantert L, Schubert JW, Jones K, Mulhearn J, Egbertson M, Meng Z, Hanney B, Gomez R, Harrison ST, McQuade P, Bueters T, Uslaner J, Morrow J, Thomson F, Kong J, Liao J, Selyutin O, Bao J, Hastings NB, Agrawal S, Magliaro BC, Monsma FJ Jr, Smith MD, Risso S, Hesk D, Hostetler E, Mazzola R. Tong L, et al. Among authors: bao j. J Med Chem. 2020 Mar 12;63(5):2411-2425. doi: 10.1021/acs.jmedchem.9b01406. Epub 2020 Mar 3. J Med Chem. 2020. PMID: 32101422 Free article.
Potent Kv1.3 inhibitors from correolide-modification of the C18 position.
Bao J, Miao S, Kayser F, Kotliar AJ, Baker RK, Doss GA, Felix JP, Bugianesi RM, Slaughter RS, Kaczorowski GJ, Garcia ML, Ha SN, Castonguay L, Koo GC, Shah K, Springer MS, Staruch MJ, Parsons WH, Rupprecht KM. Bao J, et al. Bioorg Med Chem Lett. 2005 Jan 17;15(2):447-51. doi: 10.1016/j.bmcl.2004.10.058. Bioorg Med Chem Lett. 2005. PMID: 15603971
Novel fragmentation reaction of correolide.
Bao J, Baker RK, Doss GA, Kayser F, Kotliar A, Miao S, Parsons WH, Rupprecht KM. Bao J, et al. Org Lett. 2002 May 30;4(11):1871-3. doi: 10.1021/ol020053g. Org Lett. 2002. PMID: 12027635
p38 MAP kinase inhibitors: metabolically stabilized piperidine-substituted quinolinones and naphthyridinones.
Bao J, Hunt JA, Miao S, Rupprecht KM, Stelmach JE, Liu L, Ruzek RD, Sinclair PJ, Pivnichny JV, Hop CE, Kumar S, Zaller DM, Shoop WL, O'neill EA, O'keefe SJ, Thompson CM, Cubbon RM, Wang R, Zhang WX, Thompson JE, Doherty JB. Bao J, et al. Bioorg Med Chem Lett. 2006 Jan 1;16(1):64-8. doi: 10.1016/j.bmcl.2005.09.065. Epub 2005 Oct 18. Bioorg Med Chem Lett. 2006. PMID: 16242322
Invention of MK-8262, a Cholesteryl Ester Transfer Protein (CETP) Inhibitor Backup to Anacetrapib with Best-in-Class Properties.
Vachal P, Duffy JL, Campeau LC, Amin RP, Mitra K, Murphy BA, Shao PP, Sinclair PJ, Ye F, Katipally R, Lu Z, Ondeyka D, Chen YH, Zhao K, Sun W, Tyagarajan S, Bao J, Wang SP, Cote J, Lipardi C, Metzger D, Leung D, Hartmann G, Wollenberg GK, Liu J, Tan L, Xu Y, Chen Q, Liu G, Blaustein RO, Johns DG. Vachal P, et al. Among authors: bao j. J Med Chem. 2021 Sep 23;64(18):13215-13258. doi: 10.1021/acs.jmedchem.1c00959. Epub 2021 Aug 10. J Med Chem. 2021. PMID: 34375108
Optimization of Preclinical Metabolism for Somatostatin Receptor Subtype 5-Selective Antagonists.
Liu W, Hussain Z, Zang Y, Sweis RF, Romero FA, Finke PE, Moningka R, Bao J, Plotkin MA, Shang J, Dingley KH, Salituro G, Murphy BA, Howard AD, Ujjainwalla F, Wood HB, Duffy JL. Liu W, et al. Among authors: bao j. ACS Med Chem Lett. 2018 Oct 5;9(11):1088-1093. doi: 10.1021/acsmedchemlett.8b00306. eCollection 2018 Nov 8. ACS Med Chem Lett. 2018. PMID: 30429950 Free PMC article.
Correolide and derivatives are novel immunosuppressants blocking the lymphocyte Kv1.3 potassium channels.
Koo GC, Blake JT, Shah K, Staruch MJ, Dumont F, Wunderler D, Sanchez M, McManus OB, Sirotina-Meisher A, Fischer P, Boltz RC, Goetz MA, Baker R, Bao J, Kayser F, Rupprecht KM, Parsons WH, Tong XC, Ita IE, Pivnichny J, Vincent S, Cunningham P, Hora D Jr, Feeney W, Kaczorowski G, et al. Koo GC, et al. Among authors: bao j. Cell Immunol. 1999 Nov 1;197(2):99-107. doi: 10.1006/cimm.1999.1569. Cell Immunol. 1999. PMID: 10607427
Benzamide derivatives as blockers of Kv1.3 ion channel.
Miao S, Bao J, Garcia ML, Goulet JL, Hong XJ, Kaczorowski GJ, Kayser F, Koo GC, Kotliar A, Schmalhofer WA, Shah K, Sinclair PJ, Slaughter RS, Springer MS, Staruch MJ, Tsou NN, Wong F, Parsons WH, Rupprecht KM. Miao S, et al. Among authors: bao j. Bioorg Med Chem Lett. 2003 Mar 24;13(6):1161-4. doi: 10.1016/s0960-894x(03)00014-3. Bioorg Med Chem Lett. 2003. PMID: 12643934
4,157 results