Evaluation and synthesis of 7-arylhydroxymethyltriazolopyridines as potential cardiovascular agents

被引：13

作者：

Abarca, B ^{[1
]}

Ballesteros, R

Elmasnaouy, M

D'Ocón, P

Ivorra, MD

Valiente, M

机构：

[1] Univ Valencia, Fac Farm, Dept Quim Organ, Avda Vicente Andres Estelles S-N, Valencia 46100, Spain

[2] Univ Valencia, Fac Farm, Dept Farmacol, Valencia 46100, Spain

来源：

ARKIVOC | 2002年

关键词：

triazolopyridines; lithiation reaction; alpha(1)-adrenoceptor antagonism; calcium channels blockade;

D O I：

10.3998/ark.5550190.0003.a02

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

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.

引用

页码：9 / 13

页数：5

共 6 条

[1] Triazolopyridines 21.: The stereochemistry of 1-[1,2,3]triazolo [1,5-a] pyridin-7-yl-4-(2H-[1,2,3]triazol-4-yl)-1,3-butadienes and triazolo ring opening derivatives [J].