Evaluation and synthesis of 7-arylhydroxymethyltriazolopyridines as potential cardiovascular agents

Abstract
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.
Description
Bibliographic reference
ABARCA GONZALEZ, Belen ; Ballesteros Campos,Rafael ; Elmasnaouy, Mostafá ; D’Ocón, Pilar ; Ivorra Insa, Maria Dolores ; Valiente Bautista, Miguel, 2002, Evaluation and synthesis of 7-arylhydroxymethyltriazolopyridines as potential cardiovascular agents, Arkivoc, vol. 2002, no. X, p. 9-13
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