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Page 1
Fluorinated Isoindolinone-Based Glucosylceramide Synthase Inhibitors with Low Human Dose Projections.
Loughran HM, Schirripa KM, Roecker AJ, Breslin MJ, Tong L, Fillgrove KL, Kuo Y, Bleasby K, Collier H, Altman MD, Ford MC, Newman JA, Drolet RE, Cosden M, Jinn S, Flick RB, Liu X, Minnick C, Watt ML, Lemaire W, Burlein C, Adam GC, Austin LA, Marcus JN, Smith SM, Fraley ME. Loughran HM, et al. Among authors: burlein c. ACS Med Chem Lett. 2023 Dec 21;15(1):123-131. doi: 10.1021/acsmedchemlett.3c00436. eCollection 2024 Jan 11. ACS Med Chem Lett. 2023. PMID: 38229758 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: burlein c. 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.
Discovery of a Distinct Chemical and Mechanistic Class of Allosteric HIV-1 Integrase Inhibitors with Antiretroviral Activity.
Burlein C, Wang C, Xu M, Bhatt T, Stahlhut M, Ou Y, Adam GC, Heath J, Klein DJ, Sanders J, Narayan K, Abeywickrema P, Heo MR, Carroll SS, Grobler JA, Sharma S, Diamond TL, Converso A, Krosky DJ. Burlein C, et al. ACS Chem Biol. 2017 Nov 17;12(11):2858-2865. doi: 10.1021/acschembio.7b00550. Epub 2017 Oct 19. ACS Chem Biol. 2017. PMID: 29024587
Redefining the Histone Deacetylase Inhibitor Pharmacophore: High Potency with No Zinc Cofactor Interaction.
Beshore DC, Adam GC, Barnard RJO, Burlein C, Gallicchio SN, Holloway MK, Krosky D, Lemaire W, Myers RW, Patel S, Plotkin MA, Powell DA, Rada V, Cox CD, Coleman PJ, Klein DJ, Wolkenberg SE. Beshore DC, et al. Among authors: burlein c. ACS Med Chem Lett. 2021 Mar 7;12(4):540-547. doi: 10.1021/acsmedchemlett.1c00074. eCollection 2021 Apr 8. ACS Med Chem Lett. 2021. PMID: 33854701 Free PMC article.
A novel glucosylceramide synthase inhibitor attenuates alpha synuclein pathology and lysosomal dysfunction in preclinical models of synucleinopathy.
Cosden M, Jinn S, Yao L, Gretzula CA, Kandebo M, Toolan D, Hatcher NG, Ma L, Lemaire W, Adam GC, Burlein C, Minnick C, Flick R, Watt ML, Mulhearn J, Fraley M, Drolet RE, Marcus JN, Smith SM. Cosden M, et al. Among authors: burlein c. Neurobiol Dis. 2021 Nov;159:105507. doi: 10.1016/j.nbd.2021.105507. Epub 2021 Sep 9. Neurobiol Dis. 2021. PMID: 34509608 Free article.
Pyrazole Ureas as Low Dose, CNS Penetrant Glucosylceramide Synthase Inhibitors for the Treatment of Parkinson's Disease.
Roecker AJ, Schirripa KM, Loughran HM, Tong L, Liang T, Fillgrove KL, Kuo Y, Bleasby K, Collier H, Altman MD, Ford MC, Drolet RE, Cosden M, Jinn S, Hatcher NG, Yao L, Kandebo M, Vardigan JD, Flick RB, Liu X, Minnick C, Price LA, Watt ML, Lemaire W, Burlein C, Adam GC, Austin LA, Marcus JN, Smith SM, Fraley ME. Roecker AJ, et al. Among authors: burlein c. ACS Med Chem Lett. 2023 Jan 12;14(2):146-155. doi: 10.1021/acsmedchemlett.2c00441. eCollection 2023 Feb 9. ACS Med Chem Lett. 2023. PMID: 36793422 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: burlein c. 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
Discovery of Broad-Spectrum Herpes Antiviral Oxazolidinone Amide Derivatives and Their Structure-Activity Relationships.
Plotkin MA, Labroli M, Schubert J, Shaw A, Schlegel KS, Berger R, Cooke AJ, Hayes RP, Armacost KA, Kinek K, Krosky P, Burlein C, Meng S, DiNunzio E, Murray EM, Agrawal S, Madeira M, Flattery A, Yao H, Leithead A, Rose WA 2nd, Cox C, Tellers DM, McKenna PM, Raheem I. Plotkin MA, et al. Among authors: burlein c. ACS Med Chem Lett. 2024 Jul 9;15(8):1232-1241. doi: 10.1021/acsmedchemlett.4c00117. eCollection 2024 Aug 8. ACS Med Chem Lett. 2024. PMID: 39140041
Synthesis and evaluation of imidazole acetic acid inhibitors of activated thrombin-activatable fibrinolysis inhibitor as novel antithrombotics.
Barrow JC, Nantermet PG, Stauffer SR, Ngo PL, Steinbeiser MA, Mao SS, Carroll SS, Bailey C, Colussi D, Bosserman M, Burlein C, Cook JJ, Sitko G, Tiller PR, Miller-Stein CM, Rose M, McMasters DR, Vacca JP, Selnick HG. Barrow JC, et al. Among authors: burlein c. J Med Chem. 2003 Dec 4;46(25):5294-7. doi: 10.1021/jm034141y. J Med Chem. 2003. PMID: 14640538
27 results