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Page 1
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. Among authors: dimuzio jm. 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. Among authors: dimuzio jm. 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-5172, a Macrocyclic Hepatitis C Virus NS3/4a Protease Inhibitor.
Harper S, McCauley JA, Rudd MT, Ferrara M, DiFilippo M, Crescenzi B, Koch U, Petrocchi A, Holloway MK, Butcher JW, Romano JJ, Bush KJ, Gilbert KF, McIntyre CJ, Nguyen KT, Nizi E, Carroll SS, Ludmerer SW, Burlein C, DiMuzio JM, Graham DJ, McHale CM, Stahlhut MW, Olsen DB, Monteagudo E, Cianetti S, Giuliano C, Pucci V, Trainor N, Fandozzi CM, Rowley M, Coleman PJ, Vacca JP, Summa V, Liverton NJ. Harper S, et al. Among authors: dimuzio jm. ACS Med Chem Lett. 2012 Mar 2;3(4):332-6. doi: 10.1021/ml300017p. eCollection 2012 Apr 12. ACS Med Chem Lett. 2012. PMID: 24900473 Free PMC article.
Inhibitors of the hepatitis C virus NS3 protease with basic amine functionality at the P3-amino acid N-terminus: discovery and optimization of a new series of P2-P4 macrocycles.
Harper S, Ferrara M, Crescenzi B, Pompei M, Palumbi MC, DiMuzio JM, Donghi M, Fiore F, Koch U, Liverton NJ, Pesci S, Petrocchi A, Rowley M, Summa V, Gardelli C. Harper S, et al. Among authors: dimuzio jm. J Med Chem. 2009 Aug 13;52(15):4820-37. doi: 10.1021/jm900372w. J Med Chem. 2009. PMID: 19624135
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: dimuzio jm. 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: dimuzio jm. 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.
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: dimuzio jm. 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: dimuzio j. 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
41 results