6533b854fe1ef96bd12adf1e
RESEARCH PRODUCT
Evaluation and synthesis of 7-arylhydroxymethyltriazolopyridines as potential cardiovascular agents
Belén AbarcaRafael BallesterosPilar D'oconMostafá ElmasnaouyMiguel ValienteM. Dolores Ivorrasubject
ChemistryTriazolopyridines ; Lithiation reaction ; α1-adrenoceptor antagonism ; Calcium channels blockadeUNESCO::QUÍMICACalcium channels blockade:QUÍMICA::Química orgánica [UNESCO]Organic Chemistry:QUÍMICA [UNESCO]lcsh:QD241-441lcsh:Organic chemistryCardiovascular agentTriazolopyridinesα1-adrenoceptor antagonismUNESCO::QUÍMICA::Química orgánicaLithiation reactionHumanitiesdescription
7-Arylhydroxymethyltriazolopyridines 3a-c and 4a-d were synthesized by regioselective lithiation of [1,2,3]triazolo[1,5-a]pyridines 1 and 2 and subsequent trapping of the 7-lithioderivatives formed using aryl aldehydes as electrophiles. The structural relationship between compounds 3a-c and 4a-d and arylethanolamines suggested their consideration as potential cardiovascular agents. A preliminary evaluation as vascular smooth muscle relaxants was carried out. These compounds did not act as α1-adrenoceptor antagonists and were unable to block calcium entry through voltage-dependent calcium channels. Abarca Gonzalez, Belen, Belen.Abarca@uv.es ; Ballesteros Campos, Rafael, Rafael.Ballesteros@uv.es ; Ivorra Insa, Maria Dolores, Dolores.Ivorra@uv.es ; Valiente Bautista, Miguel, Miguel.Valiente@uv.es
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2002-01-01 |