Synthesis and evaluation of uterine relaxant activity for a novel series of substituted p-hydroxyphenylethanolamines
作者:C.L. Viswanathan、A.S. Chaudhari
DOI:10.1016/j.bmc.2006.06.006
日期:2006.10
Novel racemic 1-(4-hydroxyphenyl)-2-[3-(substituted phenoxy)-2-hydroxy-1-propyl]aminopropan-1-ol hydrochlorides (9a-h) were synthesized by condensing racemic 1-(p-hydroxyphenyl)-2-aminopropan-1-ol hydrochloride (6) with substituted aryloxymethyloxiranes (8a-h) in DMF in presence of anhydrous potassium carbonate and then reacting with dry hydrogen chloride gas. They were evaluated for uterine relaxant
通过缩合外消旋1-(对羟基苯基)合成新型外消旋1-(4-羟基苯基)-2- [3-(取代苯氧基)-2-羟基-1-丙基]氨基丙烷-1-醇盐酸盐(9a-h)。 )-2-氨基丙-1-醇盐酸盐(6)在无水碳酸钾存在下于DMF中与取代的芳氧基甲基环氧乙烷(8a-h)混合,然后与干燥的氯化氢气体反应。对离体大鼠子宫的体外子宫松弛活性和妊娠大鼠体内的子宫松弛活性进行了评估。使用大鼠子宫组织匀浆通过cAMP [3H]分析研究了它们的cAMP释放潜能,并评估了狗的心脏刺激潜能。所有化合物在体外均表现出有效的子宫松弛活性,并显着延迟了妊娠大鼠的分娩。除9b和9c外,它们的cAMP释放潜能均高于盐酸异苏比林。最后,与盐酸异苏必林相比,这些化合物的心脏刺激潜力微不足道。