Synthesis and positive inotropic evaluation of 1-(benzylamino)-3-(4,5-di-hydro[1,2,4]trizaolo[4,3-a]quinolin-7-yloxy)propan-2-ol derivatives  

作　　者：Ting Ting Li Ling Zhang Zhe Shan Quan Hai Bo Zhu Hu Ri Piao 

机构地区：[1]Key Laboratory of Natural Resources and Functional Molecules of the Changbai Mountain, Affiliated Ministry of Education, Yanbian University College of Pharmacy, Yanji 133000, China [2]Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China

出　　处：《Chinese Chemical Letters》2009年第2期175-177,共3页中国化学快报（英文版）

基　　金：supported by the National Natural Science Foundation of China(No.30560177);the Natural Science Foundation of Jilin Province of China(No.20060567).

摘　　要：In an attempt to search for more potent positive inotropic agents, a series of 1-（benzylamino）-3-（4,5-dihydro[ 1,2,4]trizaolo[4,3- a]quinolin-7-yloxy）propan-2-ol derivatives was synthesized in four steps using 6-hydroxy-3,4-dihydro-2（1H）-quinolinone as a starting material, and their positive inotropic activities were evaluated by measuring the coronary blood flow （CBF） and the left ventricular pressure （LVP） followed by calculating the rate of pressure development （dp/dtmax values） in the preparation of rat Langendorff＇s heart. Three compounds （5d, 5g, 5j） showed favorable activities, among which 5g was shown the most potent with dp/dtmax value of 9.7% and CBF value of 17.8% at a concentration of 1×10^-5 mol/L in our in vitro study.In an attempt to search for more potent positive inotropic agents, a series of 1-（benzylamino）-3-（4,5-dihydro[ 1,2,4]trizaolo[4,3- a]quinolin-7-yloxy）propan-2-ol derivatives was synthesized in four steps using 6-hydroxy-3,4-dihydro-2（1H）-quinolinone as a starting material, and their positive inotropic activities were evaluated by measuring the coronary blood flow （CBF） and the left ventricular pressure （LVP） followed by calculating the rate of pressure development （dp/dtmax values） in the preparation of rat Langendorff＇s heart. Three compounds （5d, 5g, 5j） showed favorable activities, among which 5g was shown the most potent with dp/dtmax value of 9.7% and CBF value of 17.8% at a concentration of 1×10^-5 mol/L in our in vitro study.

关 键 词：3 4-Dihydro[1 2 4]trizaolo[4 3-a]quinoline Positive inotropic activity SYNTHESIS 

分 类 号：O626.323[理学—有机化学] TQ452[理学—化学]