title: Synthesis of 2-(4-substitutedmethylpiperazin-1-yl)-N-(3,4-dihydro-3-oxo-2H-benzo[b][1,4]oxazin-7-yl)acetamides and their positive inotropic evaluation.
abstract: In an attempt to search for more potent positive inotropic agents, a series of 2-(4-substitutedmethylpiperazin-1-yl)-N-(3,4-dihydro-3-oxo-2H-benzo[b][1,4]oxazin-7-yl)acetamides were synthesized and their positive inotropic activities were evaluated by measuring left atrium stroke volume on isolated rabbit heart preparations. Several compounds showed favorable activities compared with the standard drug, milrinone, among which 2-(4-(4-methylbenzyl)piperazin-1-yl)-N-(3,4-dihydro-3-oxo-2H-benzo[b][1,4]oxazin-7-yl)acetamide 4e showed the most potent activity with the 5.09+/-0.00% increased stroke volume (milrinone 1.67+/-0.64%) at a concentration of 1x10(-5)M in our in vitro study. The chronotropic effects of those compounds having significant inotropic effects were also evaluated in this work.
authors.affiliation: Key Laboratory of Natural Resources and Functional Molecules of the Changbai Mountain, Affiliated Ministry of Education, Yanbian University College of Pharmacy, Yanji, Jilin Province, PR China.
authors.forename: Xue-Kun
authors.initials: XK
authors.lastname: Liu
authors.forename: Xun
authors.initials: X
authors.lastname: Cui
authors.forename: Lan
authors.initials: L
authors.lastname: Hong
authors.forename: Liang-Peng
authors.initials: LP
authors.lastname: Sun
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* / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D016279:Atrial Function, Left / Q000187:drug effects; D002316:Cardiotonic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D006325:Heart Atria / Q000187:drug effects; D010078:Oxazines / Q000737:chemistry; D015363:Quinolones / Q000737:chemistry; D011817:Rabbits; D012015:Reference Standards; D013057:Spectrum Analysis; D013318:Stroke Volume / Q000187:drug effects
chemical_list: D000081:Acetamides; D002316:Cardiotonic Agents; D010078:Oxazines; D015363:Quinolones