2-Aryl(pyrrolidin-4-yl)acetic acids are potent agonists of sphingosine-1-phosphate (S1P) receptors

A series of 2-aryl(pyrrolidine-4-yl)acetic acids (e.g., 22g) were synthesized and evaluated as S1P receptor agonists and were found to lower peripheral lymphocyte counts in mice and to have good overall pharmacokinetic properties in rat. A series of 2-aryl(pyrrolidin-4-yl)acetic acids were synthesiz...

Ausführliche Beschreibung

Gespeichert in:

Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2006-07, Vol.16 (13), p.3564-3568
Hauptverfasser:	Yan, Lin, Budhu, Richard, Huo, Pei, Lynch, Christopher L., Hale, Jeffrey J., Mills, Sander G., Hajdu, Richard, Keohane, Carol A., Rosenbach, Mark J., Milligan, James A., Shei, Gan-Ju, Chrebet, Gary, Bergstrom, James, Card, Deborah, Mandala, Suzanne M.
Format:	Artikel
Sprache:	eng
Schlagworte:	(Pyrrolidin-4-yl)acetic acids Acetates - chemical synthesis Acetates - chemistry Acetates - pharmacology Animals Biological and medical sciences Immunomodulators Immunosuppressants Lymphocyte Count Lysophospholipids - antagonists & inhibitors Medical sciences Mice Molecular Structure Peripheral lymphocyte lowering Pharmacology. Drug treatments Protein Binding - drug effects Pyrrolidines - chemical synthesis Pyrrolidines - chemistry Pyrrolidines - pharmacology Rats Receptors, Lysosphingolipid - agonists S1P agonists Sphingosine - analogs & derivatives Sphingosine - antagonists & inhibitors Stereoisomerism Structure-Activity Relationship
Online-Zugang:	Volltext
Tags:	Tag hinzufügen Keine Tags, Fügen Sie den ersten Tag hinzu!

Beschreibung
Zusammenfassung:	A series of 2-aryl(pyrrolidine-4-yl)acetic acids (e.g., 22g) were synthesized and evaluated as S1P receptor agonists and were found to lower peripheral lymphocyte counts in mice and to have good overall pharmacokinetic properties in rat. A series of 2-aryl(pyrrolidin-4-yl)acetic acids were synthesized and their biological activities were evaluated as agonists of S1P receptors. These analogs were able to induce lowering of lymphocyte counts in the peripheral blood of mice and were found to have good overall pharmacokinetic properties in rat.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2006.03.090