We designed and synthesized 5 new compounds. Their chemical structures were confirmed by means of MS, HNMR andelemental analysis. FPA was tested for positive inotropic activity. The results showed that FPA could incre...We designed and synthesized 5 new compounds. Their chemical structures were confirmed by means of MS, HNMR andelemental analysis. FPA was tested for positive inotropic activity. The results showed that FPA could increase the contrastive amplitudeof isolated atrium of guinea pigs and had no influence upon rhythm of the hearts.展开更多
In order to search into the positive inotropic activities after a triazole ring being added to the quinoline ring,synthesis of two 4,5 dihydrotriazoloquinoline derivatives were desgned and synthesized.All of them were...In order to search into the positive inotropic activities after a triazole ring being added to the quinoline ring,synthesis of two 4,5 dihydrotriazoloquinoline derivatives were desgned and synthesized.All of them were new compounds whose structures were confirmed by MS?IR and 1H NMR.展开更多
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
Isoflavonoids possess broad activities besides cardiovascular activity.3 phenyl 4(1H)quinolinone derivatives are isosteres of isoflavonoids.They have similar spatial structures.Eight 3 phenyl 4(1H)quinolinone halide d...Isoflavonoids possess broad activities besides cardiovascular activity.3 phenyl 4(1H)quinolinone derivatives are isosteres of isoflavonoids.They have similar spatial structures.Eight 3 phenyl 4(1H)quinolinone halide derivatives were synthesised for studying their biological activities especially cardiovascular activity.Their chemical structures were confirmed by 1 H NMR,MS and IR.The preliminary tests with isolated heart of rabbits indicated that both mixtures,A 1B 1,A 2B 2,had more positive inotropic effect than vesnarinone which appeared on the market in Japanese.The results of the pharmacological tests showed that the two mixtures did not affect the blood pressure and respiration of the dogs.展开更多
文摘We designed and synthesized 5 new compounds. Their chemical structures were confirmed by means of MS, HNMR andelemental analysis. FPA was tested for positive inotropic activity. The results showed that FPA could increase the contrastive amplitudeof isolated atrium of guinea pigs and had no influence upon rhythm of the hearts.
文摘In order to search into the positive inotropic activities after a triazole ring being added to the quinoline ring,synthesis of two 4,5 dihydrotriazoloquinoline derivatives were desgned and synthesized.All of them were new compounds whose structures were confirmed by MS?IR and 1H NMR.
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.
文摘Isoflavonoids possess broad activities besides cardiovascular activity.3 phenyl 4(1H)quinolinone derivatives are isosteres of isoflavonoids.They have similar spatial structures.Eight 3 phenyl 4(1H)quinolinone halide derivatives were synthesised for studying their biological activities especially cardiovascular activity.Their chemical structures were confirmed by 1 H NMR,MS and IR.The preliminary tests with isolated heart of rabbits indicated that both mixtures,A 1B 1,A 2B 2,had more positive inotropic effect than vesnarinone which appeared on the market in Japanese.The results of the pharmacological tests showed that the two mixtures did not affect the blood pressure and respiration of the dogs.
