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-h...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.展开更多
基金supported by the National Natural Science Foundation of China(No.30560177)the Natural Science Foundation of Jilin Province of China(No.20060567).
文摘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.
