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Keywords:

  • [1,2,4]triazolo[4,3-a]quinolines;
  • 1,4-diazepan;
  • positive inotropic activity;
  • stroke volume

In an attempt to search for more potent positive inotropic agents, a series of N-(4,5-dihydro-1-methyl-[1,2,4]triazolo[4,3-a]quinolin-7-yl)-2-(substitutedbenzyl-[1,4]diazepan-1-yl)acetamides were 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 2-(4-(4-methylbenzyl)-[1,4]-diazepan-1-yl)-N-(4,5-dihydro-1-methyl-[1,2,4]triazolo[4,3-a]quinolin-7-yl)acetamide (6m) was the most potent, increasing stroke volume by 8.38 ± 0.16% (milrinone 2.45 ± 0.06%) at 3 × 10−5 m. The chronotropic effects of those compounds having inotropic effects were also evaluated in this work.