陈昌, 郑贤育, 朱佩萼, 郭惠珠. 抗疟新药的研究——具有对-氨基酚双Mannich碱的杂环化合物的合成J. 药学学报, 1982, 17(2): 112-117.
引用本文: 陈昌, 郑贤育, 朱佩萼, 郭惠珠. 抗疟新药的研究——具有对-氨基酚双Mannich碱的杂环化合物的合成J. 药学学报, 1982, 17(2): 112-117.
CHEN Chang, ZHENG Xian-yu, ZHU Pei-e , GUO Hui-zhu, . STUDIES ON NEW ANTIMALARIALS——SYNTHESIS OF HETEROCYCLIC COMPOUNDS CARRYING DOUBLE MANNICH BASIC CHAINS OF p-AMINOPHENOLJ. Acta Pharmaceutica Sinica, 1982, 17(2): 112-117.
Citation: CHEN Chang, ZHENG Xian-yu, ZHU Pei-e , GUO Hui-zhu, . STUDIES ON NEW ANTIMALARIALS——SYNTHESIS OF HETEROCYCLIC COMPOUNDS CARRYING DOUBLE MANNICH BASIC CHAINS OF p-AMINOPHENOLJ. Acta Pharmaceutica Sinica, 1982, 17(2): 112-117.

抗疟新药的研究——具有对-氨基酚双Mannich碱的杂环化合物的合成

STUDIES ON NEW ANTIMALARIALS——SYNTHESIS OF HETEROCYCLIC COMPOUNDS CARRYING DOUBLE MANNICH BASIC CHAINS OF p-AMINOPHENOL

  • 摘要: 作者等将对-氨基酚双Mannich碱的侧链与苯骈g喹啉、1,5-萘啶、吡啶骈2,3-d嘧啶,苯骈c吖啶、吡啶骈2,3-c吖啶以及吡啶骈2,3-e吖啶等杂环相连,合成了不同类型的杂环化合物V1~19。部分化合物经鼠疟Plasmodium berghei试验,发现化合物V1~3,8,10,12,18等具有杀灭红细胞内期裂殖体的作用。部分化合物用约氏原虫(P.yoelii)-斯氏按蚊(Anophelesstephensi)-鼠模型筛选,未见有明显作用。

     

    Abstract: This paper presents the preparation of heterocyclic compounds V1~19 carrying double Mannich basic side chains of p-aminophenol. These heterocyclic nuclei are benzo g quinoline, 1,5-naphthyridine, pyrido2,3-dpyrimidine, benzocacridine, pyrido2,3-c acridine and pyrido2,3-eacridine. Compounds V1~19 were synthesized from the heterocyclic intermediates a~f by condensing with p-aminophenol. Products Ⅵ carrying p-aminophenoi reacted further with Mannich reagents to yield the desired compounds.Compounds V1~3, 6, 8~15, 19 were tested for blood schizonticidal activity against Plasmodium berghei in mice. The results showed that compounds V1~3, 8, 10, 12, 19 were rather effective. In addition, compounds V4~10, 16, 19 did not show any activity in P. yoelii-Anopheles stephensi-mouse model.

     

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