Synthesis and in-vitro inotropic evaluation of 2-(4-substitutedbenzyl-1,4-diazepan-1-yl)-N-(4,5-dihydro-1-phenyl-[1,2,4]triazolo[4,3-a]quinolin-7-yl)acetamides.
We describe the synthesis and positive inotropic evaluation of a series of 2-(4-substitutedbenzyl-1,4-diazepan-1-yl)-N-(4,5-dihydro-1-phenyl-[1,2,4]triazolo[4,3-a]quinolin-7-yl)acetamides by measuring left atrial stroke volume in preparations of isolated rabbit-heart. Several compounds were developed from, and showed favorable activities compared with the standard drug milrinone. Compound 5o was the most potent with an increased stroke volume of 9.17 ± 0.14% (milrinone 2.47 ± 0.08%) at 3 × 10⁻⁵ M in our in-vitro study. The chronotropic effects of those compounds having inotropic effects were also evaluated.
Yanbian University College of Pharmacy, Yanji, PR China.
Sheng-Ming
SM
Jiang
Bai-Jun
BJ
Ye
Xue-Kun
XK
Liu
Tian-Yi
TY
Zhang
Xun
X
Cui
Hu-Ri
HR
Piao
D000081:Acetamides / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D002316:Cardiotonic Agents / Q000138:chemical synthesis*; D006321:Heart / Q000187:drug effects*; D006339:Heart Rate; D066298:In Vitro Techniques; D011804:Quinolines / Q000138:chemical synthesis* / Q000494:pharmacology; D011817:Rabbits; D013318:Stroke Volume / Q000187:drug effects*; D013329:Structure-Activity Relationship
D000081:Acetamides; D002316:Cardiotonic Agents; D011804:Quinolines