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Page 1
CCR5 antagonists: 3-(pyrrolidin-1-yl)propionic acid analogues with potent anti-HIV activity.
Lynch CL, Hale JJ, Budhu RJ, Gentry AL, Finke PE, Caldwell CG, Mills SG, MacCoss M, Shen DM, 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 E. Lynch CL, et al. Among authors: emini e. Org Lett. 2003 Jul 10;5(14):2473-5. doi: 10.1021/ol034707c. Org Lett. 2003. PMID: 12841758
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. 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. 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. 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. 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
Antagonists of human CCR5 receptor containing 4-(pyrazolyl)piperidine side chains. Part 1: Discovery and SAR study of 4-pyrazolylpiperidine side chains.
Shen DM, Shu M, Mills SG, Chapman KT, Malkowitz L, Springer MS, Gould SL, DeMartino JA, Siciliano SJ, Kwei GY, Carella A, Carver G, Holmes K, Schleif WA, Danzeisen R, Hazuda D, Kessler J, Lineberger J, Miller MD, Emini EA. Shen DM, et al. Bioorg Med Chem Lett. 2004 Feb 23;14(4):935-9. doi: 10.1016/j.bmcl.2003.12.004. Bioorg Med Chem Lett. 2004. PMID: 15012997
Antagonists of human CCR5 receptor containing 4-(pyrazolyl)piperidine side chains. Part 2: Discovery of potent, selective, and orally bioavailable compounds.
Shen DM, Shu M, Willoughby CA, Shah S, Lynch CL, Hale JJ, Mills SG, Chapman KT, Malkowitz L, Springer MS, Gould SL, DeMartino JA, Siciliano SJ, Lyons K, Pivnichny JV, Kwei GY, Carella A, Carver G, Holmes K, Schleif WA, Danzeisen R, Hazuda D, Kessler J, Lineberger J, Miller MD, Emini EA. Shen DM, et al. Bioorg Med Chem Lett. 2004 Feb 23;14(4):941-5. doi: 10.1016/j.bmcl.2003.12.005. Bioorg Med Chem Lett. 2004. PMID: 15012998
Antagonists of human CCR5 receptor containing 4-(pyrazolyl)piperidine side chains. Part 3: SAR studies on the benzylpyrazole segment.
Shu M, Loebach JL, Parker KA, Mills SG, Chapman KT, Shen DM, Malkowitz L, Springer MS, Gould SL, DeMartino JA, Siciliano SJ, Salvo JD, Lyons K, Pivnichny JV, Kwei GY, Carella A, Carver G, Holmes K, Schleif WA, Danzeisen R, Hazuda D, Kessler J, Lineberger J, Miller MD, Emini EA. Shu M, et al. Bioorg Med Chem Lett. 2004 Feb 23;14(4):947-52. doi: 10.1016/j.bmcl.2003.12.006. Bioorg Med Chem Lett. 2004. PMID: 15012999
Syntheses and SAR studies of 4-(heteroarylpiperdin-1-yl-methyl)-pyrrolidin-1-yl-acetic acid antagonists of the human CCR5 chemokine receptor.
Shankaran K, Donnelly KL, Shah SK, Guthikonda RN, MacCoss M, Mills SG, Gould SL, Malkowitz L, Siciliano SJ, Springer MS, Carella A, Carver G, Hazuda D, Holmes K, Kessler J, Lineberger J, Miller MD, Emini EA, Schleif WA. Shankaran K, et al. Bioorg Med Chem Lett. 2004 Jul 5;14(13):3419-24. doi: 10.1016/j.bmcl.2004.04.078. Bioorg Med Chem Lett. 2004. PMID: 15177445
Syntheses and biological evaluation of 5-(piperidin-1-yl)-3-phenyl-pentylsulfones as CCR5 antagonists.
Shankaran K, Donnelly KL, Shah SK, Caldwell CG, Chen P, Finke PE, Oates B, MacCoss M, Mills SG, DeMartino JA, Gould SL, Malkowitz L, Siciliano SJ, Springer MS, Kwei G, Carella A, Carver G, Danzeisen R, Hazuda D, Holmes K, Kessler J, Lineberger J, Miller MD, Emini EA, Schleif WA. Shankaran K, et al. Among authors: emini ea. Bioorg Med Chem Lett. 2004 Jul 5;14(13):3589-93. doi: 10.1016/j.bmcl.2004.03.112. Bioorg Med Chem Lett. 2004. PMID: 15177481
190 results