Synthesis and SAR evaluation of 1,2,4-triazoles as A(2A) receptor antagonists

Synthesis and SAR evaluation of 1,2,4-triazoles as A(2A) receptor antagonists

The synthesis and in vitro structure-activity relationships (SAR) of a series of triazoles as A(2A) receptor antagonists is reported. This resulted in the identification of potent, selective and permeable 1,2,4-triazoles such as 42 for further optimization and evaluation in vivo.

Gespeichert in:
Bibliographische Detailangaben
Veröffentlicht in:Bioorganic & medicinal chemistry letters 2004-02, Vol.14 (3), p.817-821
Hauptverfasser: Alanine, Alexander, Anselm, Lilli, Steward, Lucinda, Thomi, Stefan, Vifian, Walter, Groaning, Michael D
Format: Artikel
Sprache:eng
Schlagworte:
Adenosine A2 Receptor Antagonists
Animals
Cell Membrane - chemistry
In Vitro Techniques
Molecular Structure
Rats
Structure-Activity Relationship
Triazoles - chemical synthesis
Triazoles - pharmacology
Online-Zugang:Volltext
Tags: Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
Beschreibung
Zusammenfassung:The synthesis and in vitro structure-activity relationships (SAR) of a series of triazoles as A(2A) receptor antagonists is reported. This resulted in the identification of potent, selective and permeable 1,2,4-triazoles such as 42 for further optimization and evaluation in vivo.
ISSN:0960-894X
DOI:10.1016/j.bmcl.2003.09.095