title: 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.
abstract: 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 x 10(-5) M in our in-vitro study. The chronotropic effects of those compounds having inotropic effects were also evaluated in this work.
authors.affiliation: Key Laboratory of Natural Resources and Functional Molecules of Changbai Mountain, Affiliated Ministry of Education, Yanbian University College of Pharmacy, Yanji, Jilin, PR China.
authors.forename: Jing-Yuan
authors.initials: JY
authors.lastname: Li
authors.forename: Xun
authors.initials: X
authors.lastname: Cui
authors.forename: Xue-Kun
authors.initials: XK
authors.lastname: Liu
authors.forename: Lan
authors.initials: L
authors.lastname: Hong
authors.forename: Zhe-Shan
authors.initials: ZS
authors.lastname: Quan
authors.forename: Hu-Ri
authors.initials: HR
authors.lastname: Piao
mesh_terms: D000081:Acetamides / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D002316:Cardiotonic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D006321:Heart / Q000187:drug effects / Q000502:physiology; D066298:In Vitro Techniques; D011804:Quinolines / Q000138:chemical synthesis* / Q000494:pharmacology; D011817:Rabbits; D013318:Stroke Volume / Q000187:drug effects
chemical_list: D000081:Acetamides; D002316:Cardiotonic Agents; D011804:Quinolines