CCR5 receptor antagonist

Wood A, Armour D (2005) The discovery of the CCR5 receptor antagonist, UK-427,857, a new agent for the treatment of HIV infection and AIDS, Prog Med Chem 43 239-271... 

CCR5 receptor antagonists for antiviral activity 2005BML2129... 

Chemokine CCR5 receptor antagonists vicriviroc and mamviroc prevent viral entry into white blood cells. They are, respectively, undergoing Phase II and Phase III clinical trials for the treatment of HIV infection as part of polytherapies. ... 

Ghosal, A. et al., Identification of human liver cytochrome P450 enzymes involved in biotransformation of vicriviroc, a CCR5 receptor antagonist, Drug Metab. Dispos., 35(12), 2186, 2007. 

Figure 9.26 Left Epoxide hydrolase inhibitors." Right CCR5 receptor antagonists. ...

Palani, A., et al. Synthesis, SAR, and biological evaluation of oximino-piperidino-piperidine amides. 1. Orally bioavailable CCR5 receptor antagonists with potent anti-FIIV activity. J. Med. Chem. 2002, 45, 3143-3160. 

Scheme 26 Reductive amination for a CCR5 receptor antagonist (Roche)...

Roche [66] was also successful in implementing a quite rare reductive amination reaction for the synthesis of a CCR5 receptor antagonist using ammonium acetate as nitrogen source (Scheme 26). While catalyst activity was on the low side, excellent ee was achieved. 

Molecular Interactions and Binding Modes of CCR5 Receptor Antagonists 225... 

Hale, J.J. et al. (2001) 1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 2 lead optimization affording selective, orally bioavailable compounds with potent Anti-HIV activity. Bioorgank S, Medkirud Chemistry Letters, 11 (20), 2741-2745. 

Kim, D. et al. (2005) Potent 1,3,4-trisubstituted pyrrolidine CCR5 receptor antagonists effects of fused heterocydes on antiviral activity and pharmacokinetic properties. Bioorgank Medkirud Chemistry Letters, 15 (8), 2129-2134. 

Armour, Duncan, de Groot, MarcelJ., Edwards, Martin, Perros, Manos, Price, DavidA., Stammen, BlandaL, and Wood, Anthony (2006) The discovery of CCR5 receptor antagonists for the treatment of HIV infection Hit-to-Lead studies. ChemMedChem, 1 (7), 706-709. 

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