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Page 1
Cyclopentane-based human NK1 antagonists. Part 1: discovery and initial SAR.
Finke PE, Meurer LC, Levorse DA, Mills SG, Maccoss M, Sadowski S, Cascieri MA, Tsao KL, Chicchi GG, Metzger JM, Macintyre DE. Finke PE, et al. Among authors: cascieri ma. Bioorg Med Chem Lett. 2006 Sep 1;16(17):4497-503. doi: 10.1016/j.bmcl.2006.06.035. Epub 2006 Jul 7. Bioorg Med Chem Lett. 2006. PMID: 16824752
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: cascieri ma. 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
Spirocyclic NK(1) antagonists II: [4.5]-spiroethers.
Williams BJ, Cascieri MA, Chicchi GG, Harrison T, Owens AP, Owen SN, Rupniak NM, Tattersall DF, Williams A, Swain CJ. Williams BJ, et al. Among authors: cascieri ma. Bioorg Med Chem Lett. 2002 Oct 7;12(19):2719-22. doi: 10.1016/s0960-894x(02)00509-7. Bioorg Med Chem Lett. 2002. PMID: 12217362
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: cascieri ma. 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
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: cascieri ma. 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
Cyclopentane-based human NK1 antagonists. Part 2: development of potent, orally active, water-soluble derivatives.
Meurer LC, Finke PE, Owens KA, Tsou NN, Ball RG, Mills SG, Maccoss M, Sadowski S, Cascieri MA, Tsao KL, Chicchi GG, Egger LA, Luell S, Metzger JM, Macintyre DE, Rupniak NM, Williams AR, Hargreaves RJ. Meurer LC, et al. Among authors: cascieri ma. Bioorg Med Chem Lett. 2006 Sep 1;16(17):4504-11. doi: 10.1016/j.bmcl.2006.06.044. Epub 2006 Jul 10. Bioorg Med Chem Lett. 2006. PMID: 16831551
Design, synthesis, and structure-activity relationship of novel CCR2 antagonists.
Kothandaraman S, Donnely KL, Butora G, Jiao R, Pasternak A, Morriello GJ, Goble SD, Zhou C, Mills SG, Maccoss M, Vicario PP, Ayala JM, Demartino JA, Struthers M, Cascieri MA, Yang L. Kothandaraman S, et al. Among authors: cascieri ma. Bioorg Med Chem Lett. 2009 Mar 15;19(6):1830-4. doi: 10.1016/j.bmcl.2008.12.050. Epub 2008 Dec 24. Bioorg Med Chem Lett. 2009. PMID: 19237282
135 results