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Synthesis and structure-activity relationships of azamacrocyclic C-X-C chemokine receptor 4 antagonists: analogues containing a single azamacrocyclic ring are potent inhibitors of T-cell tropic (X4) HIV-1 replication.
Bridger GJ, Skerlj RT, Hernandez-Abad PE, Bogucki DE, Wang Z, Zhou Y, Nan S, Boehringer EM, Wilson T, Crawford J, Metz M, Hatse S, Princen K, De Clercq E, Schols D. Bridger GJ, et al. Among authors: skerlj rt. J Med Chem. 2010 Feb 11;53(3):1250-60. doi: 10.1021/jm901530b. J Med Chem. 2010. PMID: 20043638
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. 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
Design and synthesis of pyridin-2-yloxymethylpiperidin-1-ylbutyl amide CCR5 antagonists that are potent inhibitors of M-tropic (R5) HIV-1 replication.
Skerlj R, Bridger G, Zhou Y, Bourque E, Langille J, Di Fluri M, Bogucki D, Yang W, Li T, Wang L, Nan S, Baird I, Metz M, Darkes M, Labrecque J, Lau G, Fricker S, Huskens D, Schols D. Skerlj R, et al. Bioorg Med Chem Lett. 2011 Apr 15;21(8):2450-5. doi: 10.1016/j.bmcl.2011.02.058. Epub 2011 Feb 23. Bioorg Med Chem Lett. 2011. PMID: 21398122
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. 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. 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. 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.
45 results