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2008 1
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2015 2
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Page 1
Indole acids as a novel PDE2 inhibitor chemotype that demonstrate pro-cognitive activity in multiple species.
Stachel SJ, Egbertson MS, Wai J, Machacek M, Toolan DM, Swestock J, Eddins DM, Puri V, McGaughey G, Su HP, Perlow D, Wang D, Ma L, Parthasarathy G, Reid JC, Abeywickrema PD, Smith SM, Uslaner JM. Stachel SJ, et al. Among authors: swestock j. Bioorg Med Chem Lett. 2018 Apr 1;28(6):1122-1126. doi: 10.1016/j.bmcl.2018.01.039. Epub 2018 Feb 10. Bioorg Med Chem Lett. 2018. PMID: 29534798
Discovery of vaniprevir (MK-7009), a macrocyclic hepatitis C virus NS3/4a protease inhibitor.
McCauley JA, McIntyre CJ, Rudd MT, Nguyen KT, Romano JJ, Butcher JW, Gilbert KF, Bush KJ, Holloway MK, Swestock J, Wan BL, Carroll SS, DiMuzio JM, Graham DJ, Ludmerer SW, Mao SS, Stahlhut MW, Fandozzi CM, Trainor N, Olsen DB, Vacca JP, Liverton NJ. McCauley JA, et al. Among authors: swestock j. J Med Chem. 2010 Mar 25;53(6):2443-63. doi: 10.1021/jm9015526. J Med Chem. 2010. PMID: 20163176
P2-quinazolinones and bis-macrocycles as new templates for next-generation hepatitis C virus NS3/4a protease inhibitors: discovery of MK-2748 and MK-6325.
Rudd MT, Butcher JW, Nguyen KT, McIntyre CJ, Romano JJ, Gilbert KF, Bush KJ, Liverton NJ, Holloway MK, Harper S, Ferrara M, DiFilippo M, Summa V, Swestock J, Fritzen J, Carroll SS, Burlein C, DiMuzio JM, Gates A, Graham DJ, Huang Q, McClain S, McHale C, Stahlhut MW, Black S, Chase R, Soriano A, Fandozzi CM, Taylor A, Trainor N, Olsen DB, Coleman PJ, Ludmerer SW, McCauley JA. Rudd MT, et al. Among authors: swestock j. ChemMedChem. 2015 Apr;10(4):727-35. doi: 10.1002/cmdc.201402558. Epub 2015 Mar 10. ChemMedChem. 2015. PMID: 25759009
Methyl-substitution of an iminohydantoin spiropiperidine β-secretase (BACE-1) inhibitor has a profound effect on its potency.
Egbertson M, McGaughey GB, Pitzenberger SM, Stauffer SR, Coburn CA, Stachel SJ, Yang W, Barrow JC, Neilson LA, McWherter M, Perlow D, Fahr B, Munshi S, Allison TJ, Holloway K, Selnick HG, Yang Z, Swestock J, Simon AJ, Sankaranarayanan S, Colussi D, Tugusheva K, Lai MT, Pietrak B, Haugabook S, Jin L, Chen IW, Holahan M, Stranieri-Michener M, Cook JJ, Vacca J, Graham SL. Egbertson M, et al. Among authors: swestock j. Bioorg Med Chem Lett. 2015 Nov 1;25(21):4812-4819. doi: 10.1016/j.bmcl.2015.06.082. Epub 2015 Jun 29. Bioorg Med Chem Lett. 2015. PMID: 26195137
First demonstration of cerebrospinal fluid and plasma A beta lowering with oral administration of a beta-site amyloid precursor protein-cleaving enzyme 1 inhibitor in nonhuman primates.
Sankaranarayanan S, Holahan MA, Colussi D, Crouthamel MC, Devanarayan V, Ellis J, Espeseth A, Gates AT, Graham SL, Gregro AR, Hazuda D, Hochman JH, Holloway K, Jin L, Kahana J, Lai MT, Lineberger J, McGaughey G, Moore KP, Nantermet P, Pietrak B, Price EA, Rajapakse H, Stauffer S, Steinbeiser MA, Seabrook G, Selnick HG, Shi XP, Stanton MG, Swestock J, Tugusheva K, Tyler KX, Vacca JP, Wong J, Wu G, Xu M, Cook JJ, Simon AJ. Sankaranarayanan S, et al. Among authors: swestock j. J Pharmacol Exp Ther. 2009 Jan;328(1):131-40. doi: 10.1124/jpet.108.143628. Epub 2008 Oct 14. J Pharmacol Exp Ther. 2009. PMID: 18854490
Discovery of MK-1220: A Macrocyclic Inhibitor of Hepatitis C Virus NS3/4A Protease with Improved Preclinical Plasma Exposure.
Rudd MT, McCauley JA, Butcher JW, Romano JJ, McIntyre CJ, Nguyen KT, Gilbert KF, Bush KJ, Holloway MK, Swestock J, Wan BL, Carroll SS, DiMuzio JM, Graham DJ, Ludmerer SW, Stahlhut MW, Fandozzi CM, Trainor N, Olsen DB, Vacca JP, Liverton NJ. Rudd MT, et al. Among authors: swestock j. ACS Med Chem Lett. 2011 Jan 12;2(3):207-12. doi: 10.1021/ml1002426. eCollection 2011 Mar 10. ACS Med Chem Lett. 2011. PMID: 24900304 Free PMC article.
Evolution of tertiary carbinamine BACE-1 inhibitors: Abeta reduction in rhesus CSF upon oral dosing.
Nantermet PG, Rajapakse HA, Stanton MG, Stauffer SR, Barrow JC, Gregro AR, Moore KP, Steinbeiser MA, Swestock J, Selnick HG, Graham SL, McGaughey GB, Colussi D, Lai MT, Sankaranarayanan S, Simon AJ, Munshi S, Cook JJ, Holahan MA, Michener MS, Vacca JP. Nantermet PG, et al. Among authors: swestock j. ChemMedChem. 2009 Jan;4(1):37-40. doi: 10.1002/cmdc.200800308. ChemMedChem. 2009. PMID: 19085994 No abstract available.