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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: caldwell cg. 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
Binding of 2-aryl-4-(piperidin-1-yl)butanamines and 1,3,4-trisubstituted pyrrolidines to human CCR5: a molecular modeling-guided mutagenesis study of the binding pocket.
Castonguay LA, Weng Y, Adolfsen W, Di Salvo J, Kilburn R, Caldwell CG, Daugherty BL, Finke PE, Hale JJ, Lynch CL, Mills SG, MacCoss M, Springer MS, DeMartino JA. Castonguay LA, et al. Among authors: caldwell cg. Biochemistry. 2003 Feb 18;42(6):1544-50. doi: 10.1021/bi026639s. Biochemistry. 2003. PMID: 12578367
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: caldwell cg. Org Lett. 2003 Jul 10;5(14):2473-5. doi: 10.1021/ol034707c. Org Lett. 2003. PMID: 12841758
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: caldwell cg. 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
Discovery of human CCR5 antagonists containing hydantoins for the treatment of HIV-1 infection.
Kim D, Wang L, Caldwell CG, Chen P, Finke PE, Oates B, MacCoss M, Mills SG, Malkowitz L, Gould SL, DeMartino JA, Springer MS, Hazuda D, Miller M, Kessler J, Danzeisen R, Carver G, Carella A, Holmes K, Lineberger J, Schleif WA, Emini EA. Kim D, et al. Among authors: caldwell cg. Bioorg Med Chem Lett. 2001 Dec 17;11(24):3099-102. doi: 10.1016/s0960-894x(01)00654-0. Bioorg Med Chem Lett. 2001. PMID: 11720851
Design, synthesis, and SAR of heterocycle-containing antagonists of the human CCR5 receptor for the treatment of HIV-1 infection.
Kim D, Wang L, Caldwell CG, Chen P, Finke PE, Oates B, MacCoss M, Mills SG, Malkowitz L, Gould SL, DeMartino JA, Springer MS, Hazuda D, Miller M, Kessler J, Danzeisen R, Carver G, Carella A, Holmes K, Lineberger J, Schleif WA, Emini EA. Kim D, et al. Among authors: caldwell cg. Bioorg Med Chem Lett. 2001 Dec 17;11(24):3103-6. doi: 10.1016/s0960-894x(01)00655-2. Bioorg Med Chem Lett. 2001. PMID: 11720852
Substituted 4,6-diaminoquinolines as inhibitors of C5a receptor binding.
Lanza TJ, Durette PL, Rollins T, Siciliano S, Cianciarulo DN, Kobayashi SV, Caldwell CG, Springer MS, Hagmann WK. Lanza TJ, et al. Among authors: caldwell cg. J Med Chem. 1992 Jan 24;35(2):252-8. doi: 10.1021/jm00080a008. J Med Chem. 1992. PMID: 1310118
Substituted 2-aminopyridines as inhibitors of nitric oxide synthases.
Hagmann WK, Caldwell CG, Chen P, Durette PL, Esser CK, Lanza TJ, Kopka IE, Guthikonda R, Shah SK, MacCoss M, Chabin RM, Fletcher D, Grant SK, Green BG, Humes JL, Kelly TM, Luell S, Meurer R, Moore V, Pacholok SG, Pavia T, Williams HR, Wong KK. Hagmann WK, et al. Among authors: caldwell cg. Bioorg Med Chem Lett. 2000 Sep 4;10(17):1975-8. doi: 10.1016/s0960-894x(00)00389-9. Bioorg Med Chem Lett. 2000. PMID: 10987430
29 results