Premium
Synthesis and Positive Inotropic Evaluation of ( E )‐2‐(4‐Cinnamylpiperazin‐1‐yl)‐ N ‐(1‐substituted‐4,5‐dihydro‐[1,2,4]triazolo[4,3‐a]quinolin‐7‐yl)acetamides
Author(s) -
Wu Yan,
Ma LongXu,
Niu TianWei,
Meng FanLing,
Cui Xun,
Piao HuRi
Publication year - 2012
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.201200159
Subject(s) - milrinone , chronotropic , inotrope , acetamide , chemistry , atrium (architecture) , stroke volume , pharmacology , stereochemistry , heart rate , cardiology , medicine , atrial fibrillation , blood pressure , organic chemistry
A series of ( E )‐2‐(4‐cinnamylpiperazin‐1‐yl)‐ N ‐(1‐substituted‐4,5‐dihydro‐[1,2,4]triazolo[4,3‐a]quinolin‐7‐yl)acetamides were synthesized and evaluated for their positive inotropic activity by measuring the left atrium stroke volume on isolated rabbit heart preparations. This class of compounds presented favorable in vitro activity compared with the standard drug, milrinone, among which N ‐(1‐(3‐chlorophenyl)‐4,5‐dihydro‐[1,2,4]triazolo[4,3‐a]quinolin‐7‐yl)‐2‐(4‐cinnamylpiperazin‐1‐yl)acetamide 5e was found to be the most potent with 16.58 ± 0.11% increased stroke volume (milrinone: 2.46 ± 0.07%) at a concentration of 3 × 10 −5 M. The chronotropic effects of the compounds having inotropic effects were also evaluated.