title: 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.
abstract: 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.
authors.affiliation: Key Laboratory of Natural Resources and Functional Molecules of the Changbai Mountain, Affiliated Ministry of Education, Yanbian University College of Pharmacy, Yanji 133000, P. R. China.
authors.forename: Yan
authors.initials: Y
authors.lastname: Wu
authors.forename: Long-Xu
authors.initials: LX
authors.lastname: Ma
authors.forename: Tian-Wei
authors.initials: TW
authors.lastname: Niu
authors.forename: Fan-Ling
authors.initials: FL
authors.lastname: Meng
authors.forename: Xun
authors.initials: X
authors.lastname: Cui
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*; D066298:In Vitro Techniques; D015394:Molecular Structure; D011804:Quinolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011817:Rabbits; D013318:Stroke Volume / Q000187:drug effects; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
chemical_list: D000081:Acetamides; D002316:Cardiotonic Agents; D011804:Quinolines; D014230:Triazoles