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Page 1
Novel Pan-Coronavirus 3CL Protease Inhibitor MK-7845: Biological and Pharmacological Profiling.
Alvarez N, Adam GC, Howe JA, Sharma V, Zimmerman MD, Dolgov E, Rasheed R, Nizar F, Sahay K, Nelson AM, Park S, Zhou X, Burlein C, Fay JF, Iwamoto DV, Bahnck-Teets CM, Getty KL, Lin Goh S, Salhab I, Smith K, Boyce CW, Cabalu TD, Murgolo N, Fox NG, Mayhood TW, Shurtleff VW, Layton ME, Parish CA, McCauley JA, Olsen DB, Perlin DS. Alvarez N, et al. Among authors: mccauley ja. Viruses. 2024 Jul 18;16(7):1158. doi: 10.3390/v16071158. Viruses. 2024. PMID: 39066320 Free PMC article.
Invention of MK-7845, a SARS-CoV-2 3CL Protease Inhibitor Employing a Novel Difluorinated Glutamine Mimic.
Shurtleff VW, Layton ME, Parish CA, Perkins JJ, Schreier JD, Wang Y, Adam GC, Alvarez N, Bahmanjah S, Bahnck-Teets CM, Boyce CW, Burlein C, Cabalu TD, Campbell BT, Carroll SS, Chang W, de Lera Ruiz M, Dolgov E, Fay JF, Fox NG, Goh SL, Hartingh TJ, Hurzy DM, Kelly MJ 3rd, Klein DJ, Klingler FM, Krishnamurthy H, Kudalkar S, Mayhood TW, McKenna PM, Murray EM, Nahas D, Nawrat CC, Park S, Qian D, Roecker AJ, Sharma V, Shipe WD, Su J, Taggart RV, Truong Q, Wu Y, Zhou X, Zhuang N, Perlin DS, Olsen DB, Howe JA, McCauley JA. Shurtleff VW, et al. Among authors: mccauley ja. J Med Chem. 2024 Mar 14;67(5):3935-3958. doi: 10.1021/acs.jmedchem.3c02248. Epub 2024 Feb 16. J Med Chem. 2024. PMID: 38365209
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: mccauley ja. 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.
Discovery of MK-8718, an HIV Protease Inhibitor Containing a Novel Morpholine Aspartate Binding Group.
Bungard CJ, Williams PD, Ballard JE, Bennett DJ, Beaulieu C, Bahnck-Teets C, Carroll SS, Chang RK, Dubost DC, Fay JF, Diamond TL, Greshock TJ, Hao L, Holloway MK, Felock PJ, Gesell JJ, Su HP, Manikowski JJ, McKay DJ, Miller M, Min X, Molinaro C, Moradei OM, Nantermet PG, Nadeau C, Sanchez RI, Satyanarayana T, Shipe WD, Singh SK, Truong VL, Vijayasaradhi S, Wiscount CM, Vacca JP, Crane SN, McCauley JA. Bungard CJ, et al. Among authors: mccauley ja. ACS Med Chem Lett. 2016 May 9;7(7):702-7. doi: 10.1021/acsmedchemlett.6b00135. eCollection 2016 Jul 14. ACS Med Chem Lett. 2016. PMID: 27437081 Free PMC article.
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: mccauley ja. 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.
Design and Synthesis of Piperazine Sulfonamide Cores Leading to Highly Potent HIV-1 Protease Inhibitors.
Bungard CJ, Williams PD, Schulz J, Wiscount CM, Holloway MK, Loughran HM, Manikowski JJ, Su HP, Bennett DJ, Chang L, Chu XJ, Crespo A, Dwyer MP, Keertikar K, Morriello GJ, Stamford AW, Waddell ST, Zhong B, Hu B, Ji T, Diamond TL, Bahnck-Teets C, Carroll SS, Fay JF, Min X, Morris W, Ballard JE, Miller MD, McCauley JA. Bungard CJ, et al. Among authors: mccauley ja. ACS Med Chem Lett. 2017 Nov 13;8(12):1292-1297. doi: 10.1021/acsmedchemlett.7b00386. eCollection 2017 Dec 14. ACS Med Chem Lett. 2017. PMID: 29259750 Free PMC article.
The Invention of WM382, a Highly Potent PMIX/X Dual Inhibitor toward the Treatment of Malaria.
de Lera Ruiz M, Favuzza P, Guo Z, Zhao L, Hu B, Lei Z, Zhan D, Murgolo N, Boyce CW, Vavrek M, Thompson J, Ngo A, Jarman KE, Robbins J, Boddey J, Sleebs BE, Lowes KN, Cowman AF, Olsen DB, McCauley JA. de Lera Ruiz M, et al. Among authors: mccauley ja. ACS Med Chem Lett. 2022 Oct 12;13(11):1745-1754. doi: 10.1021/acsmedchemlett.2c00355. eCollection 2022 Nov 10. ACS Med Chem Lett. 2022. PMID: 36385924 Free PMC article.
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: mccauley ja. 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.
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: mccauley ja. ChemMedChem. 2015 Apr;10(4):727-35. doi: 10.1002/cmdc.201402558. Epub 2015 Mar 10. ChemMedChem. 2015. PMID: 25759009
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: mccauley ja. 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.
46 results