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喹啉酮衍生物的合成及其心血管活性
引用本文:王晓莉,徐鸣夏,李瑞雪,蔡绍辉.喹啉酮衍生物的合成及其心血管活性[J].化学研究与应用,2003,15(2):280-281,F003.
作者姓名:王晓莉  徐鸣夏  李瑞雪  蔡绍辉
作者单位:1. 四川大学华西医学院,四川,成都,610041
2. 四川大学华西药学院,四川,成都,610041
摘    要:异黄酮化合物具有心血管活性1],雌激素活性2]及抗骨质疏松3]活性等。3 苯基 4(1H)喹啉酮衍生物是异黄酮化合物的等电子体,文献报道它具有与异黄酮化合物相似的心血管活性4]和抗肿瘤5]活性。结构中具有氟原子的化合物大多能改善脂溶性,增强生理活性,且能选择性作用于脑细胞及脑血管;喹诺酮类抗菌药中具有优良抗菌活性的化合物几乎都含有氟原子。我们对含氟的3 苯基 4(1H)喹啉酮类化合物进行了研究。以氟氯苯胺为原料,合成了其7 氯衍生物(化合物A1~A4),及5 氯衍生物(化合物B1~B4),其中7 氯衍生物为主产物,合成路线如下:化合…

关 键 词:喹啉酮衍生物  合成  心血管活性  3-苯基-4(1H)喹啉酮  抗菌药  抗菌活性
文章编号:1004-1656(2003)02-0280-03

Synthesis and cardiovascular activities of 3-pheny1-4(1H)quinolinone halide derivatives
WANG Xiao li ,XU Ming xia ,LI Rui xue ,CAI Shao hui.Synthesis and cardiovascular activities of 3-pheny1-4(1H)quinolinone halide derivatives[J].Chemical Research and Application,2003,15(2):280-281,F003.
Authors:WANG Xiao li  XU Ming xia  LI Rui xue  CAI Shao hui
Institution:WANG Xiao li 1,XU Ming xia 1,LI Rui xue 1,CAI Shao hui 2
Abstract: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.
Keywords:3phenyl  4(1H)quinolinone derivatives  cardiovascular activity  positive inotropic activity  synthesis
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