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.
Alanine
Alexander
A
F Hoffmann-La Roche AG, Pharmaceuticals Division, Discovery Chemistry, Lead Generation, Basel CH 4070, Switzerland.
Anselm
Lilli
L
Steward
Lucinda
L
Thomi
Stefan
S
Vifian
Walter
W
Groaning
Michael D
MD
D058917:Adenosine A2 Receptor Antagonists; D000818:Animals; D002462:Cell Membrane / Q000737:chemistry*; D066298:In Vitro Techniques; D015394:Molecular Structure; D051381:Rats; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000138:chemical synthesis* / Q000494:pharmacology*
D058917:Adenosine A2 Receptor Antagonists; D014230:Triazoles; C045575:1,2,4-triazole