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Chiral N,N-disubstituted trifluoro-3-amino-2-propanols are potent inhibitors of cholesteryl ester transfer protein.
J Med Chem. 2002 Aug 29;45(18):3891-904. doi: 10.1021/jm020038h.
J Med Chem. 2002.
PMID: 12190312
Discovery of a simple picomolar inhibitor of cholesteryl ester transfer protein.
Reinhard EJ, Wang JL, Durley RC, Fobian YM, Grapperhaus ML, Hickory BS, Massa MA, Norton MB, Promo MA, Tollefson MB, Vernier WF, Connolly DT, Witherbee BJ, Melton MA, Regina KJ, Smith ME, Sikorski JA.
Reinhard EJ, et al. Among authors: grapperhaus ml.
J Med Chem. 2003 May 22;46(11):2152-68. doi: 10.1021/jm020528+.
J Med Chem. 2003.
PMID: 12747787
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Stereospecific inhibition of CETP by chiral N,N-disubstituted trifluoro-3-amino-2-propanols.
Connolly DT, Witherbee BJ, Melton MA, Durley RC, Grapperhaus ML, McKinnis BR, Vernier WF, Babler MA, Shieh JJ, Smith ME, Sikorski JA.
Connolly DT, et al. Among authors: grapperhaus ml.
Biochemistry. 2000 Nov 14;39(45):13870-9. doi: 10.1021/bi001356q.
Biochemistry. 2000.
PMID: 11076528
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Discovery of chiral N,N-disubstituted trifluoro-3-amino-2-propanols as potent inhibitors of cholesteryl ester transfer protein.
Durley RC, Grapperhaus ML, Massa MA, Mischke DA, Parnas BL, Fobian YM, Rath NP, Honda DD, Zeng M, Connolly DT, Heuvelman DM, Witherbee BJ, Glenn KC, Krul ES, Smith ME, Sikorski JA.
Durley RC, et al. Among authors: grapperhaus ml.
J Med Chem. 2000 Nov 30;43(24):4575-8. doi: 10.1021/jm000337b.
J Med Chem. 2000.
PMID: 11101348
No abstract available.
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Discovery of N-(4-Fluoro-3-methoxybenzyl)-6-(2-(((2S,5R)-5-(hydroxymethyl)-1,4-dioxan-2-yl)methyl)-2H-tetrazol-5-yl)-2-methylpyrimidine-4-carboxamide. A Highly Selective and Orally Bioavailable Matrix Metalloproteinase-13 Inhibitor for the Potential Treatment of Osteoarthritis.
Ruminski PG, Massa M, Strohbach J, Hanau CE, Schmidt M, Scholten JA, Fletcher TR, Hamper BC, Carroll JN, Shieh HS, Caspers N, Collins B, Grapperhaus M, Palmquist KE, Collins J, Baldus JE, Hitchcock J, Kleine HP, Rogers MD, McDonald J, Munie GE, Messing DM, Portolan S, Whiteley LO, Sunyer T, Schnute ME.
Ruminski PG, et al.
J Med Chem. 2016 Jan 14;59(1):313-27. doi: 10.1021/acs.jmedchem.5b01434. Epub 2015 Dec 24.
J Med Chem. 2016.
PMID: 26653735
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Discovery of 2-chloro-N-((4,4-difluoro-1-hydroxycyclohexyl)methyl)-5-(5-fluoropyrimidin-2-yl)benzamide as a potent and CNS penetrable P2X7 receptor antagonist.
Chen X, Pierce B, Naing W, Grapperhaus ML, Phillion DP.
Chen X, et al. Among authors: grapperhaus ml.
Bioorg Med Chem Lett. 2010 May 15;20(10):3107-11. doi: 10.1016/j.bmcl.2010.03.094. Epub 2010 Mar 30.
Bioorg Med Chem Lett. 2010.
PMID: 20392639
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Aminopyrazole Carboxamide Bruton's Tyrosine Kinase Inhibitors. Irreversible to Reversible Covalent Reactive Group Tuning.
Schnute ME, Benoit SE, Buchler IP, Caspers N, Grapperhaus ML, Han S, Hotchandani R, Huang N, Hughes RO, Juba BM, Kim KH, Liu E, McCarthy E, Messing D, Miyashiro JS, Mohan S, O'Connell TN, Ohren JF, Parikh MD, Schmidt M, Selness SR, Springer JR, Thanabal V, Trujillo JI, Walker DP, Wan ZK, Withka JM, Wittwer AJ, Wood NL, Xing L, Zapf CW, Douhan J 3rd.
Schnute ME, et al. Among authors: grapperhaus ml.
ACS Med Chem Lett. 2018 Dec 3;10(1):80-85. doi: 10.1021/acsmedchemlett.8b00461. eCollection 2019 Jan 10.
ACS Med Chem Lett. 2018.
PMID: 30655951
Free PMC article.
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