title: Synthesis and SAR evaluation of 1,2,4-triazoles as A(2A) receptor antagonists.
abstract: 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.
authors.affiliation: F Hoffmann-La Roche AG, Pharmaceuticals Division, Discovery Chemistry, Lead Generation, Basel CH 4070, Switzerland.
authors.forename: Alexander
authors.initials: A
authors.lastname: Alanine
authors.forename: Lilli
authors.initials: L
authors.lastname: Anselm
authors.forename: Lucinda
authors.initials: L
authors.lastname: Steward
authors.forename: Stefan
authors.initials: S
authors.lastname: Thomi
authors.forename: Walter
authors.initials: W
authors.lastname: Vifian
authors.forename: Michael D
authors.initials: MD
authors.lastname: Groaning
mesh_terms: 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*
chemical_list: D058917:Adenosine A2 Receptor Antagonists; D014230:Triazoles; C045575:1,2,4-triazole