臺灣博碩士論文加值系統

本論文設計合成一系列可能具有降血壓,抗血小板凝集之含有苯并咪■及
■喏■之Mannich鹽基衍生物.以對甲氧苯胺為起始反應物進行,乙醯化,硝
化,水解,環化及去甲基反應可得2-取代5-■基苯并咪■及2,3-二取代6-■
基■喏■中間產物.而後再進行Mannich反應,得Mannich鹽基終產物2-取
代-4-二烷胺甲基-5-■基苯并咪■,2,3-二取代5-二烷胺甲基-6-■基■喏
■計終產物計二十五種.生物活性試驗,使用先天性高血壓大白鼠經週邊給
藥,SD( Sprague-Dawley)大白鼠經中樞給藥,評估藥物對實驗動物血壓與
心跳之變化;以兔子靜脈抽出之血液,加入不同誘導血小板凝集之試劑再施
以藥物,評估藥物抑制血小板凝集之活性.初步之藥理試驗結果顯示,2-苯
基-4-(1-■咯啶甲基)-5-■基苯并咪■(46a),2-苯基-4-(1-六氫■啶甲
基)-5-■基苯并咪■ (46b),2-苯基-4-(1-嗎福■甲基)-5-■基苯并咪
■(46c),具有明顯抗凝血活性;2-苯基-4-[1-(2-甲基苯)-六氫■啶甲基
]-5-■基苯并咪■(46d),2,3-二甲基-5-[1-(2-甲基苯)-六氫■■甲基
]-6-■喏■

The objective of this study is to design and synthesize some
novel derivatives of benimidazole and quinoxaline, containing
Mannich base, with potential vasodilation and antiaggregation
activities. p-Ansidine was used as a starting material for
acetylation, nitration, hydrolysis, cyclization and
demethylation. Further manipulations by Mannich reaction arious
end products. Twenty-five new products have been successfully
prepared in this laboratory. The end products were tested, in
vivo, in spontaneously hypertensive and Sprague-Dawley rats to
evaluates their possible hypotensive effect. The in vitro
antiaggregation was conducted in the veins of the rabbit blood.
2-Phenyl-4-(1-pyrrolidinylmethyl)-5- hydroxybenzimidazole(46
a),2-phenyl-4-(1-piperidylmethyl)- 5-hydroxybenzimidazole(46
b),2-phenyl-4-(morphinylmethyl)- 5-hydroxydenizimdazole(46c)
were most potent in the antiaggregation test. 2-Phenyl-4-[1-(2-
methoxyphenyl)- piperazylmethyl]-5-hydroxybenzimidazole(46
d),2,3-dimethyl- 5-[1-(2-methoxyphenyl)-piperazylmethyl]-6-
hydroxyquinoxaline(49d) were potent antihypertensive drugs.