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Page 1
Design of novel CXCR4 antagonists that are potent inhibitors of T-tropic (X4) HIV-1 replication.
Skerlj R, Bridger G, McEachern E, Harwig C, Smith C, Kaller A, Veale D, Yee H, Skupinska K, Wauthy R, Wang L, Baird I, Zhu Y, Burrage K, Yang W, Sartori M, Huskens D, De Clercq E, Schols D. Skerlj R, et al. Among authors: mceachern e. Bioorg Med Chem Lett. 2011 Mar 1;21(5):1414-8. doi: 10.1016/j.bmcl.2011.01.021. Epub 2011 Jan 11. Bioorg Med Chem Lett. 2011. PMID: 21295470
Design and synthesis of pyridin-2-ylmethylaminopiperidin-1-ylbutyl amide CCR5 antagonists that are potent inhibitors of M-tropic (R5) HIV-1 replication.
Skerlj R, Bridger G, Zhou Y, Bourque E, McEachern E, Langille J, Harwig C, Veale D, Yang W, Li T, Zhu Y, Bey M, Baird I, Sartori M, Metz M, Mosi R, Nelson K, Bodart V, Wong R, Fricker S, Mac Farland R, Huskens D, Schols D. Skerlj R, et al. Among authors: mceachern e. Bioorg Med Chem Lett. 2011 Dec 1;21(23):6950-4. doi: 10.1016/j.bmcl.2011.09.133. Epub 2011 Oct 8. Bioorg Med Chem Lett. 2011. PMID: 22033460
Design of substituted imidazolidinylpiperidinylbenzoic acids as chemokine receptor 5 antagonists: potent inhibitors of R5 HIV-1 replication.
Skerlj R, Bridger G, Zhou Y, Bourque E, McEachern E, Metz M, Harwig C, Li TS, Yang W, Bogucki D, Zhu Y, Langille J, Veale D, Ba T, Bey M, Baird I, Kaller A, Krumpak M, Leitch D, Satori M, Vocadlo K, Guay D, Nan S, Yee H, Crawford J, Chen G, Wilson T, Carpenter B, Gauthier D, Macfarland R, Mosi R, Bodart V, Wong R, Fricker S, Schols D. Skerlj R, et al. Among authors: mceachern e. J Med Chem. 2013 Oct 24;56(20):8049-65. doi: 10.1021/jm401101p. Epub 2013 Oct 3. J Med Chem. 2013. PMID: 24090135
Mitigating hERG Inhibition: Design of Orally Bioavailable CCR5 Antagonists as Potent Inhibitors of R5 HIV-1 Replication.
Skerlj R, Bridger G, Zhou Y, Bourque E, McEachern E, Danthi S, Langille J, Harwig C, Veale D, Carpenter B, Ba T, Bey M, Baird I, Wilson T, Metz M, MacFarland R, Mosi R, Bodart V, Wong R, Fricker S, Huskens D, Schols D. Skerlj R, et al. Among authors: mceachern e. ACS Med Chem Lett. 2012 Jan 25;3(3):216-21. doi: 10.1021/ml2002604. eCollection 2012 Mar 8. ACS Med Chem Lett. 2012. PMID: 24900457 Free PMC article.
Synthesis and SAR of novel CXCR4 antagonists that are potent inhibitors of T tropic (X4) HIV-1 replication.
Skerlj R, Bridger G, McEachern E, Harwig C, Smith C, Wilson T, Veale D, Yee H, Crawford J, Skupinska K, Wauthy R, Yang W, Zhu Y, Bogucki D, Di Fluri M, Langille J, Huskens D, De Clercq E, Schols D. Skerlj R, et al. Among authors: mceachern e. Bioorg Med Chem Lett. 2011 Jan 1;21(1):262-6. doi: 10.1016/j.bmcl.2010.11.023. Epub 2010 Nov 6. Bioorg Med Chem Lett. 2011. PMID: 21109432
Discovery of novel small molecule orally bioavailable C-X-C chemokine receptor 4 antagonists that are potent inhibitors of T-tropic (X4) HIV-1 replication.
Skerlj RT, Bridger GJ, Kaller A, McEachern EJ, Crawford JB, Zhou Y, Atsma B, Langille J, Nan S, Veale D, Wilson T, Harwig C, Hatse S, Princen K, De Clercq E, Schols D. Skerlj RT, et al. Among authors: mceachern ej. J Med Chem. 2010 Apr 22;53(8):3376-88. doi: 10.1021/jm100073m. J Med Chem. 2010. PMID: 20297846
Discovery of MK-8719, a Potent O-GlcNAcase Inhibitor as a Potential Treatment for Tauopathies.
Selnick HG, Hess JF, Tang C, Liu K, Schachter JB, Ballard JE, Marcus J, Klein DJ, Wang X, Pearson M, Savage MJ, Kaul R, Li TS, Vocadlo DJ, Zhou Y, Zhu Y, Mu C, Wang Y, Wei Z, Bai C, Duffy JL, McEachern EJ. Selnick HG, et al. Among authors: mceachern ej. J Med Chem. 2019 Nov 27;62(22):10062-10097. doi: 10.1021/acs.jmedchem.9b01090. Epub 2019 Sep 29. J Med Chem. 2019. PMID: 31487175
MK-8719, a Novel and Selective O-GlcNAcase Inhibitor That Reduces the Formation of Pathological Tau and Ameliorates Neurodegeneration in a Mouse Model of Tauopathy.
Wang X, Li W, Marcus J, Pearson M, Song L, Smith K, Terracina G, Lee J, Hong KK, Lu SX, Hyde L, Chen SC, Kinsley D, Melchor JP, Rubins DJ, Meng X, Hostetler E, Sur C, Zhang L, Schachter JB, Hess JF, Selnick HG, Vocadlo DJ, McEachern EJ, Uslaner JM, Duffy JL, Smith SM. Wang X, et al. Among authors: mceachern ej. J Pharmacol Exp Ther. 2020 Aug;374(2):252-263. doi: 10.1124/jpet.120.266122. Epub 2020 Jun 3. J Pharmacol Exp Ther. 2020. PMID: 32493725
36 results