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212 results

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Page 1
Discovery of 3,5-bis(trifluoromethyl)benzyl L-arylglycinamide based potent CCR2 antagonists.
Yang L, Zhou C, Guo L, Morriello G, Butora G, Pasternak A, Parsons WH, Mills SG, MacCoss M, Vicario PP, Zweerink H, Ayala JM, Goyal S, Hanlon WA, Cascieri MA, Springer MS. Yang L, et al. Among authors: springer ms. Bioorg Med Chem Lett. 2006 Jul 15;16(14):3735-9. doi: 10.1016/j.bmcl.2006.04.045. Epub 2006 May 15. Bioorg Med Chem Lett. 2006. PMID: 16698264
CCR5 antagonists: bicyclic isoxazolidines as conformationally constrained N-1-substituted pyrrolidines.
Lynch CL, Gentry AL, Hale JJ, Mills SG, MacCoss M, Malkowitz L, Springer MS, Gould SL, DeMartino JA, Siciliano SJ, Cascieri MA, Doss G, Carella A, Carver G, Holmes K, Schleif WA, Danzeisen R, Hazuda D, Kessler J, Lineberger J, Miller M, Emini EA. Lynch CL, et al. Among authors: springer ms. Bioorg Med Chem Lett. 2002 Feb 25;12(4):677-9. doi: 10.1016/s0960-894x(01)00835-6. Bioorg Med Chem Lett. 2002. PMID: 11844699
1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 3: polar functionality and its effect on anti-HIV-1 activity.
Hale JJ, Budhu RJ, Mills SG, MacCoss M, Gould SL, DeMartino JA, Springer MS, Siciliano SJ, Malkowitz L, Schleif WA, Hazuda D, Miller M, Kessler J, Danzeisen R, Holmes K, Lineberger J, Carella A, Carver G, Emini EA. Hale JJ, et al. Among authors: springer ms. Bioorg Med Chem Lett. 2002 Oct 21;12(20):2997-3000. doi: 10.1016/s0960-894x(02)00605-4. Bioorg Med Chem Lett. 2002. PMID: 12270192
1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 4: synthesis of N-1 acidic functionality affording analogues with enhanced antiviral activity against HIV.
Lynch CL, Hale JJ, Budhu RJ, Gentry AL, Mills SG, Chapman KT, MacCoss M, Malkowitz L, Springer MS, Gould SL, DeMartino JA, Siciliano SJ, Cascieri MA, Carella A, Carver G, Holmes K, Schleif WA, Danzeisen R, Hazuda D, Kessler J, Lineberger J, Miller M, Emini EA. Lynch CL, et al. Among authors: springer ms. Bioorg Med Chem Lett. 2002 Oct 21;12(20):3001-4. doi: 10.1016/s0960-894x(02)00606-6. Bioorg Med Chem Lett. 2002. PMID: 12270193
1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists: modifications of the arylpropylpiperidine side chains.
Lynch CL, Willoughby CA, Hale JJ, Holson EJ, Budhu RJ, Gentry AL, Rosauer KG, Caldwell CG, Chen P, Mills SG, MacCoss M, Berk S, Chen L, Chapman KT, Malkowitz L, Springer MS, Gould SL, DeMartino JA, Siciliano SJ, Cascieri MA, Carella A, Carver G, Holmes K, Schleif WA, Danzeisen R, Hazuda D, Kessler J, Lineberger J, Miller M, Emini EA. Lynch CL, et al. Among authors: springer ms. Bioorg Med Chem Lett. 2003 Jan 6;13(1):119-23. doi: 10.1016/s0960-894x(02)00829-6. Bioorg Med Chem Lett. 2003. PMID: 12467630
1,3,4 Trisubstituted pyrrolidine CCR5 receptor antagonists bearing 4-aminoheterocycle substituted piperidine side chains.
Willoughby CA, Rosauer KG, Hale JJ, Budhu RJ, Mills SG, Chapman KT, MacCoss M, Malkowitz L, Springer MS, Gould SL, DeMartino JA, Siciliano SJ, Cascieri MA, Carella A, Carver G, Holmes K, Schleif WA, Danzeisen R, Hazuda D, Kessler J, Lineberger J, Miller M, Emini EA. Willoughby CA, et al. Among authors: springer ms. Bioorg Med Chem Lett. 2003 Feb 10;13(3):427-31. doi: 10.1016/s0960-894x(02)00988-5. Bioorg Med Chem Lett. 2003. PMID: 12565944
Potent 1,3,4-trisubstituted pyrrolidine CCR5 receptor antagonists: effects of fused heterocycles on antiviral activity and pharmacokinetic properties.
Kim D, Wang L, Hale JJ, Lynch CL, Budhu RJ, Maccoss M, Mills SG, Malkowitz L, Gould SL, DeMartino JA, Springer MS, Hazuda D, Miller M, Kessler J, Hrin RC, Carver G, Carella A, Henry K, Lineberger J, Schleif WA, Emini EA. Kim D, et al. Among authors: springer ms. Bioorg Med Chem Lett. 2005 Apr 15;15(8):2129-34. doi: 10.1016/j.bmcl.2005.02.030. Bioorg Med Chem Lett. 2005. PMID: 15808483
Antagonists of the human CCR5 receptor as anti-HIV-1 agents. part 1: discovery and initial structure-activity relationships for 1 -amino-2-phenyl-4-(piperidin-1-yl)butanes.
Dorn CP, Finke PE, Oates B, Budhu RJ, Mills SG, MacCoss M, Malkowitz L, Springer MS, Daugherty BL, Gould SL, DeMartino JA, Siciliano SJ, Carella A, Carver G, Holmes K, Danzeisen R, Hazuda D, Kessler J, Lineberger J, Miller M, Schleif WA, Emini EA. Dorn CP, et al. Among authors: springer ms. Bioorg Med Chem Lett. 2001 Jan 22;11(2):259-64. doi: 10.1016/s0960-894x(00)00637-5. Bioorg Med Chem Lett. 2001. PMID: 11206473
Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 2: structure-activity relationships for substituted 2-Aryl-1-[N-(methyl)-N-(phenylsulfonyl)amino]-4-(piperidin-1-yl)butanes.
Finke PE, Meurer LC, Oates B, Mills SG, MacCoss M, Malkowitz L, Springer MS, Daugherty BL, Gould SL, DeMartino JA, Siciliano SJ, Carella A, Carver G, Holmes K, Danzeisen R, Hazuda D, Kessler J, Lineberger J, Miller M, Schleif WA, Emini EA. Finke PE, et al. Among authors: springer ms. Bioorg Med Chem Lett. 2001 Jan 22;11(2):265-70. doi: 10.1016/s0960-894x(00)00639-9. Bioorg Med Chem Lett. 2001. PMID: 11206474
212 results