Potent 1,3,4-trisubstituted pyrrolidine CCR5 receptor antagonists: effects of fused heterocycles on antiviral activity and pharmacokinetic properties

[Display omitted] A series of 1,3,4-trisubstituted pyrrolidine CCR5 receptor antagonists containing a variety of fused heterocycles at the 4-position of the piperidine side chain has been discovered, which are orally bioavailable with potent anti-HIV activity.

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2005-04, Vol.15 (8), p.2129-2134
Hauptverfasser:	Kim, Dooseop, Wang, Liping, Hale, Jeffrey J., Lynch, Christopher L., Budhu, Richard J., MacCoss, Malcolm, Mills, Sander G., Malkowitz, Lorraine, Gould, Sandra L., DeMartino, Julie A., Springer, Martin S., Hazuda, Daria, Miller, Michael, Kessler, Joseph, Hrin, Renee C., Carver, Gwen, Carella, Anthony, Henry, Karen, Lineberger, Janet, Schleif, William A., Emini, Emilio A.
Format:	Artikel
Sprache:	eng
Schlagworte:	Administration, Oral Animals Anti-HIV Agents - chemistry Anti-HIV Agents - pharmacokinetics Antibiotics. Antiinfectious agents. Antiparasitic agents Antiviral Antiviral agents Biological and medical sciences CCR5 CCR5 Receptor Antagonists Fused heterocycles HeLa Cells Heterocyclic Compounds - chemistry Heterocyclic Compounds - pharmacokinetics HIV-1 Humans Medical sciences Pharmacology. Drug treatments Pyrrolidines - chemistry Pyrrolidines - pharmacokinetics Rats Receptors, CCR5 - metabolism
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Beschreibung
Zusammenfassung:	[Display omitted] A series of 1,3,4-trisubstituted pyrrolidine CCR5 receptor antagonists containing a variety of fused heterocycles at the 4-position of the piperidine side chain has been discovered, which are orally bioavailable with potent anti-HIV activity.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2005.02.030