Evaluation and synthesis of 7-arylhydroxymethyltriazolopyridines as potential cardiovascular agents

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 aryl ethanol amines suggested their consideration as potential cardiovascular agents. A preliminary evaluation as vascular smooth muscle relaxants was carried out. These compounds did not act as alpha(1)-adrenoceptor antagonists and were unable to block calcium entry through voltage-dependent calcium channels.