444886-13-9Relevant academic research and scientific papers
CCR5 antagonists: bicyclic isoxazolidines as conformationally constrained N-1-substituted pyrrolidines.
Lynch, Christopher L,Gentry, Amy L,Hale, Jeffrey J,Mills, Sander G,MacCoss, Malcolm,Malkowitz, Lorraine,Springer, Martin S,Gould, Sandra L,DeMartino, Julie A,Siciliano, Salvatore J,Cascieri, Margaret A,Doss, George,Carella, Anthony,Carver, Gwen,Holmes, Karen,Schleif, William A,Danzeisen, Renee,Hazuda, Daria,Kessler, Joseph,Lineberger, Janet,Miller, Michael,Emini, Emilio A
, p. 677 - 679 (2002)
A series of CCR5 antagonists containing bicyclic isoxazolidines was generated through a nitrone mediated cycloaddition with olefins bearing the preferred pharmacophores previously described. Potent antagonists (3 and 16) were generated with enhanced affinity for the CCR5 receptor while maintaining antiviral activity against HIV.
