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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: huskens d. 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
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: huskens d. 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 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: huskens d. 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-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. Among authors: huskens d. 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
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: huskens d. 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.
The molecular pharmacology of AMD11070: an orally bioavailable CXCR4 HIV entry inhibitor.
Mosi RM, Anastassova V, Cox J, Darkes MC, Idzan SR, Labrecque J, Lau G, Nelson KL, Patel K, Santucci Z, Wong RS, Skerlj RT, Bridger GJ, Huskens D, Schols D, Fricker SP. Mosi RM, et al. Among authors: huskens d. Biochem Pharmacol. 2012 Feb 15;83(4):472-9. doi: 10.1016/j.bcp.2011.11.020. Epub 2011 Nov 28. Biochem Pharmacol. 2012. PMID: 22146583
68 results