臺灣博碩士論文加值系統

本論文以五種不同磺胺氯衍生物反應，生成系列之磺胺終產物。其中二類
胺是以乙醯苯胺為起始原料，合成 6-(4-胺基苯)-4,5-二氫-3(2H)-嗒■
酮；另一類是以乙醯胺酚合成4-[2-■基-3-[4-(2-甲氧苯基)-六氫■
■-1-基-丙氧]苯胺。合成產物可能具甲型交感神經阻斷劑、磷酸二酯■
、或其他具有降壓、抗凝血潛能結構之混成產物。合計終產物為30個。生
物活性試驗使用自發性高血壓鼠，評估中樞、週邊降壓活性。以兔子靜脈
抽出之血液，施以藥物後加入不同誘導血小板凝集之試劑，評估體外藥物
抑制血小板之活性；體內試驗是評估藥物對小鼠尾部出血時間之影響。初
步之藥理試驗結果顯示，N-[4-(5,6-二氫-4-氧-嗒■-1-基取代磺胺衍生
物中，以2-■磺醯基 22c、苯磺醯基 22e、對甲苯磺醯基 22f、甲基磺醯
基 22g、異丙磺醯基 22h取代之降壓活性最佳，但以第三丁基苯磺醯基
22d與苯磺醯基 22e取代則活性消失。所有N-[[2-■基-3-[4-(2-甲氧苯
基)六氫■■-1-基]-丙氧]苯基]取代磺胺衍生物中 (29 a-e)，皆具明顯
降壓活性。

In the thesis, we conjugated five kinds of amines and various
of sulfonyl chloride by sulfonaton. Thirty new products were
successfully prepared in these experiments. All the target
compounds comprise a sulfonamido functionality which might
posses potential antihypertension and antiplatelet activities.
All the end products prepared were tested, in vivo, for
antiaggregation with rabbit blood. Blood from the tails of ICR
mice was used to test the bleeding time. N-[4-(5,6-dihydro-4-
oxo-pyridazin-1-yl)]-phenyl substituted sulfonamides exhibited
significant antihypertensive activity, especially in
benzenesulfonamides such as 22c, 22e, 22f and some simple
alkyl- sulfonamides such as 22g and 22h. In assition, this
series of compounds were most potent in antiaggregation tests,
except for 22d and 22e. All of the N-[[2-hydroxy-3-[4-(2-
methoxyphenyl) piperazin-1-yl]propoxy]phenyl] substituted
sulfonamides 29 a-h exhibited extremely potent antihypertentive
activity.