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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: emini ea. 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
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. Org Lett. 2003 Jul 10;5(14):2473-5. doi: 10.1021/ol034707c. Org Lett. 2003. PMID: 12841758
Indinavir analogues with blocked metabolism sites as HIV protease inhibitors with improved pharmacological profiles and high potency against PI-resistant viral strains.
Cheng Y, Zhang F, Rano TA, Lu Z, Schleif WA, Gabryelski L, Olsen DB, Stahlhut M, Rutkowski CA, Lin JH, Jin L, Emini EA, Chapman KT, Tata JR. Cheng Y, et al. Among authors: emini ea. Bioorg Med Chem Lett. 2002 Sep 2;12(17):2419-22. doi: 10.1016/s0960-894x(02)00424-9. Bioorg Med Chem Lett. 2002. PMID: 12161147
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: emini ea. 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: 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: emini ea. 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
190 results