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SAR of tertiary carbinamine derived BACE1 inhibitors: role of aspartate ligand amine pKa in enzyme inhibition.
Rajapakse HA, Nantermet PG, Selnick HG, Barrow JC, McGaughey GB, Munshi S, Lindsley SR, Young MB, Ngo PL, Holloway MK, Lai MT, Espeseth AS, Shi XP, Colussi D, Pietrak B, Crouthamel MC, Tugusheva K, Huang Q, Xu M, Simon AJ, Kuo L, Hazuda DJ, Graham S, Vacca JP. Rajapakse HA, et al. Among authors: holloway mk. Bioorg Med Chem Lett. 2010 Mar 15;20(6):1885-9. doi: 10.1016/j.bmcl.2010.01.137. Epub 2010 Feb 4. Bioorg Med Chem Lett. 2010. PMID: 20176482
4-Aryl-2,4-dioxobutanoic acid inhibitors of HIV-1 integrase and viral replication in cells.
Wai JS, Egbertson MS, Payne LS, Fisher TE, Embrey MW, Tran LO, Melamed JY, Langford HM, Guare JP Jr, Zhuang L, Grey VE, Vacca JP, Holloway MK, Naylor-Olsen AM, Hazuda DJ, Felock PJ, Wolfe AL, Stillmock KA, Schleif WA, Gabryelski LJ, Young SD. Wai JS, et al. Among authors: holloway mk. J Med Chem. 2000 Dec 28;43(26):4923-6. doi: 10.1021/jm000176b. J Med Chem. 2000. PMID: 11150161 No abstract available.
Identification of MK-944a: a second clinical candidate from the hydroxylaminepentanamide isostere series of HIV protease inhibitors.
Dorsey BD, McDonough C, McDaniel SL, Levin RB, Newton CL, Hoffman JM, Darke PL, Zugay-Murphy JA, Emini EA, Schleif WA, Olsen DB, Stahlhut MW, Rutkowski CA, Kuo LC, Lin JH, Chen IW, Michelson SR, Holloway MK, Huff JR, Vacca JP. Dorsey BD, et al. Among authors: holloway mk. J Med Chem. 2000 Sep 7;43(18):3386-99. doi: 10.1021/jm9903848. J Med Chem. 2000. PMID: 10978186
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: holloway mk. 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.
61 results