Synthesis and inotropic evaluation of 1-substituted-N-(4,5-dihydro-1-methyl-[1,2,4]triazolo[4,3-a]quinolin-7-yl)piperidine-4-carboxamides.
A series of 1-substituted-N-(4,5-dihydro-1-methyl-[1,2,4]triazolo[4,3-a]quinolin-7-yl) piperidine-4-carboxamides has been synthesized and evaluated for positive inotropic activity by measuring left atrium stroke volume in isolated rabbit-heart preparations. Some of these derivatives exhibited favorable activity compared with the standard drug, milrinone, among which 1-(2-fluorobenzyl)-N-(4,5-dihydro-1-methyl-[1,2,4]triazolo[4,3-a]quinolin-7-yl)piperidine-4-carboxamide 6a was the most potent, increasing stroke volume by 11.92+/-0.35% (milrinone: 6.36+/-0.13%) at 1x10(-4)M.
Changbai Mountain Key Laboratory of Natural Resources and Functional Molecules, Affiliated Ministry of Education, Yanbian University College of Pharmacy, Yanji 133000, PR China.
Ji-Yong
JY
Liu
Hai-Ling
HL
Yu
Zhe-Shan
ZS
Quan
Xun
X
Cui
Hu-Ri
HR
Piao
D000818:Animals; D002316:Cardiotonic Agents / Q000138:chemical synthesis / Q000494:pharmacology; D002625:Chemistry, Organic / Q000379:methods*; D002626:Chemistry, Pharmaceutical / Q000379:methods; D015195:Drug Design; D006321:Heart / Q000187:drug effects*; D007540:Isonipecotic Acids / Q000737:chemistry; D020105:Milrinone / Q000138:chemical synthesis / Q000494:pharmacology; D008956:Models, Chemical; D009206:Myocardium / Q000378:metabolism; D010880:Piperidines / Q000737:chemistry*; D011804:Quinolines / Q000737:chemistry*; D011817:Rabbits
D002316:Cardiotonic Agents; D007540:Isonipecotic Acids; D010880:Piperidines; D011804:Quinolines; C032727:piperidine; D020105:Milrinone