周义清, 李国福, 钟景星, 董正福, 高徐生. 2,4-二氨基-6-取代氨基磺酰喹唑啉类化合物抗鼠疟作用的研究J. 药学学报, 1984, 19(4): 245-250.
引用本文: 周义清, 李国福, 钟景星, 董正福, 高徐生. 2,4-二氨基-6-取代氨基磺酰喹唑啉类化合物抗鼠疟作用的研究J. 药学学报, 1984, 19(4): 245-250.
ZHOU Yi-qing, LI Guo-fu, ZHONG Jing-xing, DONG Zheng-fu , GAO Xu-sheng, . ANTIMALARIAL ACTIVITY OF SOME 2,4-DIAMINO-6-SUBSTITUTED AMINO SULFONYL QUINAZOLINE DERIVATIVESJ. Acta Pharmaceutica Sinica, 1984, 19(4): 245-250.
Citation: ZHOU Yi-qing, LI Guo-fu, ZHONG Jing-xing, DONG Zheng-fu , GAO Xu-sheng, . ANTIMALARIAL ACTIVITY OF SOME 2,4-DIAMINO-6-SUBSTITUTED AMINO SULFONYL QUINAZOLINE DERIVATIVESJ. Acta Pharmaceutica Sinica, 1984, 19(4): 245-250.

2,4-二氨基-6-取代氨基磺酰喹唑啉类化合物抗鼠疟作用的研究

ANTIMALARIAL ACTIVITY OF SOME 2,4-DIAMINO-6-SUBSTITUTED AMINO SULFONYL QUINAZOLINE DERIVATIVES

  • 摘要: 用伯氏鼠疟模型筛选了17个2,4-二氨基-6-取代氨基磺酰喹唑啉类化合物。初步结果显示,化合物Ⅰ4,Ⅰ5,Ⅰ10,Ⅰ11和Ⅰ12口服有较好抗疟作用,对正常敏感株(N)的SD50为0.43~2.4mg/kg×4d,高度抗氯喹株(RC)为0.19~0.42mg/kg×4d,(NK65)株为7.2~100mg/kg×4d,抗磺胺株(ORA)为11~76 mg/kg×4d。上述结果表明,该类化合物对(RC)株的疗效显著优于(N)株,但对(NK65)株的疗效较差,与磺胺类药物有轻度交叉抗性。

     

    Abstract: Seventeen 2,4-diamino-6-substituted amino sulfonyl quinazoline derivatives were tested for antimalarial activity on mice infected with several strains of Plasmodium berghei. In preliminary experiments, compounds I4, I5,I10, I11 and I12 showed marked antimalarial activity. The SDs0 of these compounds against infections with N strain were 0.43~2.4 mg/kg×4d, PO; with NK65 strain 7.2~100 mg/kg×4d, PO; with chloroquine resistant RC line 0.19~0.42 mg/kg×4d, PO; and with sulfonamide resistant ORA Iine 11~76 mg/kg×4d, PO.These results indicate that there is no cross resistance between these compounds and chloroquine. The RC line was shown to be more sensitive than the N strain. Some degree of cross resistance exists between these compounds and sulfonamides.

     

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