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Page 1
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. ChemMedChem. 2015 Apr;10(4):727-35. doi: 10.1002/cmdc.201402558. Epub 2015 Mar 10. ChemMedChem. 2015. PMID: 25759009
Molecular modeling based approach to potent P2-P4 macrocyclic inhibitors of hepatitis C NS3/4A protease.
Liverton NJ, Holloway MK, McCauley JA, Rudd MT, Butcher JW, Carroll SS, DiMuzio J, Fandozzi C, Gilbert KF, Mao SS, McIntyre CJ, Nguyen KT, Romano JJ, Stahlhut M, Wan BL, Olsen DB, Vacca JP. Liverton NJ, et al. Among authors: rudd mt. J Am Chem Soc. 2008 Apr 9;130(14):4607-9. doi: 10.1021/ja711120r. Epub 2008 Mar 14. J Am Chem Soc. 2008. PMID: 18338894
Bismacrocyclic inhibitors of hepatitis C NS3/4a protease.
McCauley JA, Rudd MT, Nguyen KT, McIntyre CJ, Romano JJ, Bush KJ, Varga SL, Ross CW 3rd, Carroll SS, DiMuzio J, Stahlhut MW, Olsen DB, Lyle TA, Vacca JP, Liverton NJ. McCauley JA, et al. Among authors: rudd mt. Angew Chem Int Ed Engl. 2008;47(47):9104-7. doi: 10.1002/anie.200803298. Angew Chem Int Ed Engl. 2008. PMID: 18925594 No abstract available.
MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
Liverton NJ, Carroll SS, Dimuzio J, Fandozzi C, Graham DJ, Hazuda D, Holloway MK, Ludmerer SW, McCauley JA, McIntyre CJ, Olsen DB, Rudd MT, Stahlhut M, Vacca JP. Liverton NJ, et al. Among authors: rudd mt. Antimicrob Agents Chemother. 2010 Jan;54(1):305-11. doi: 10.1128/AAC.00677-09. Epub 2009 Oct 19. Antimicrob Agents Chemother. 2010. PMID: 19841155 Free PMC article.
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: rudd mt. J Med Chem. 2010 Mar 25;53(6):2443-63. doi: 10.1021/jm9015526. J Med Chem. 2010. PMID: 20163176
MK-5172, a selective inhibitor of hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants.
Summa V, Ludmerer SW, McCauley JA, Fandozzi C, Burlein C, Claudio G, Coleman PJ, Dimuzio JM, Ferrara M, Di Filippo M, Gates AT, Graham DJ, Harper S, Hazuda DJ, Huang Q, McHale C, Monteagudo E, Pucci V, Rowley M, Rudd MT, Soriano A, Stahlhut MW, Vacca JP, Olsen DB, Liverton NJ, Carroll SS. Summa V, et al. Among authors: rudd mt. Antimicrob Agents Chemother. 2012 Aug;56(8):4161-7. doi: 10.1128/AAC.00324-12. Epub 2012 May 21. Antimicrob Agents Chemother. 2012. PMID: 22615282 Free PMC article.
Development of potent macrocyclic inhibitors of genotype 3a HCV NS3/4A protease.
Rudd MT, McCauley JA, Romano JJ, Butcher JW, Bush K, McIntyre CJ, Nguyen KT, Gilbert KF, Lyle TA, Holloway MK, Wan BL, Vacca JP, Summa V, Harper S, Rowley M, Carroll SS, Burlein C, DiMuzio JM, Gates A, Graham DJ, Huang Q, Ludmerer SW, McClain S, McHale C, Stahlhut M, Fandozzi C, Taylor A, Trainor N, Olsen DB, Liverton NJ. Rudd MT, et al. Bioorg Med Chem Lett. 2012 Dec 1;22(23):7201-6. doi: 10.1016/j.bmcl.2012.08.106. Epub 2012 Sep 7. Bioorg Med Chem Lett. 2012. PMID: 23021993
Development of macrocyclic inhibitors of HCV NS3/4A protease with cyclic constrained P2-P4 linkers.
Rudd MT, McIntyre CJ, Romano JJ, Butcher JW, Holloway MK, Bush K, Nguyen KT, Gilbert KF, Lyle TA, Liverton NJ, Wan BL, Summa V, Harper S, Rowley M, Vacca JP, Carroll SS, Burlein C, DiMuzio JM, Gates A, Graham DJ, Huang Q, Ludmerer SW, McClain S, McHale C, Stahlhut M, Fandozzi C, Taylor A, Trainor N, Olsen DB, McCauley JA. Rudd MT, et al. Bioorg Med Chem Lett. 2012 Dec 1;22(23):7207-13. doi: 10.1016/j.bmcl.2012.09.061. Epub 2012 Oct 2. Bioorg Med Chem Lett. 2012. PMID: 23084906
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. 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.
32 results