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Synthesis and Positive Inotropic Evaluation of 2‐(4‐(4‐Substituted benzyloxy)‐3‐methoxybenzyl)‐1,4‐diazepan‐1‐yl)‐ N ‐(4,5‐dihydro‐1‐methyl[1,2,4]triazolo[4,3‐ a ]quinolin‐7‐yl)‐acetamides
Author(s) -
Li JingYuan,
Cui Xun,
Liu XueKun,
Hong Lan,
Quan ZheShan,
Piao HuRi
Publication year - 2008
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.200800132
Subject(s) - inotrope , chemistry , stereochemistry , medicine
In an attempt to search for more potent positive inotropic agents, a series of 2‐(4‐(4‐substituted benzyloxy)‐3‐methoxybenzyl)‐1,4‐diazepan‐1‐yl)‐ N ‐(4,5‐dihydro‐1‐methyl[1,2,4]triazolo[4,3‐ a ]quinolin‐7‐yl)acetamides was synthesized and their positive inotropic activities were 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 2‐(4‐(4‐(2‐chlorobenzyloxy)‐3‐methoxybenzyl)‐1,4‐diazepan‐1‐yl)‐ N ‐(4,5‐dihydro‐1‐methyl‐[1,2,4]triazolo[4,3‐ a ]quinolin‐7‐yl)acetamide 6e was found to have the most desirable potency with the 6.79 ± 0.18% increased stroke volume (Milrinone: 1.67 ± 0.64%) at a concentration of 1×10 –5 M in our in‐vitro study. The chronotropic effects of those compounds having inotropic effects were also evaluated in this work.