Synthesis and positive inotropic activity of N-(4,5-dihydro-[1,2,4]triazolo[4,3-a]quinolin-7-yl)-2-(piperazin-1-yl)acetamide derivatives.
A series of N-(4,5-dihydro-[1,2,4]triazolo[4,3-a]quinolin-7-yl)-2-(piperazin-1-yl)acetamide derivatives were synthesized and their positive inotropic activity was evaluated by measuring left atrium stroke volume on isolated rabbit heart preparations. Several compounds showed favorable activity compared with the standard drug, milrinone, among which N-(1-benzyl-4,5-dihydro-[1,2,4]triazolo[4,3-a]quinolin-7-yl)-2-(4-benzylpiperazin-1-yl)acetamide 6j was found to be the most potent with the 13.2% increased stroke volume (milrinone 4.7%) at concentration of 3x10(-5) M in our in vitro study. The chronotropic effects of those compounds having inotropic effects were also evaluated in this work.
Zhang
Chun-Bo
CB
Key Laboratory of Natural Resources and Functional Molecules of the Changbai Mountain, Yanbian University, Ministry of Education, Yanji, Jilin 133002, PR China.
Cui
Xun
X
Hong
Lan
L
Quan
Zhe-Shan
ZS
Piao
Hu-Ri
HR
D000081:Acetamides / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D002316:Cardiotonic Agents / Q000138:chemical synthesis / Q000494:pharmacology; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D015195:Drug Design; D006321:Heart / Q000187:drug effects*; D006325:Heart Atria / Q000187:drug effects; D006339:Heart Rate / Q000187:drug effects; D020105:Milrinone / Q000494:pharmacology; D008956:Models, Chemical; D009206:Myocardium / Q000378:metabolism*; D023303:Oxazolidinones / Q000494:pharmacology; D011817:Rabbits; D013318:Stroke Volume / Q000187:drug effects; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000138:chemical synthesis* / Q000494:pharmacology
D000081:Acetamides; D002316:Cardiotonic Agents; D023303:Oxazolidinones; D014230:Triazoles; D020105:Milrinone