周昭武, 刘镇固, 戴昌世, 马立人. 抗辐射药物的研究:硫辛酸氨基酯的合成J. 药学学报, 1984, 19(10): 742-747.
引用本文: 周昭武, 刘镇固, 戴昌世, 马立人. 抗辐射药物的研究:硫辛酸氨基酯的合成J. 药学学报, 1984, 19(10): 742-747.
ZHOU Zhao-Wu, LIU Zhen-Gu, DAI Chang-Shi, MA Li-Ren. STUDIES ON ANTIRADIATION DRUG: SYNTHESIS OF AMINO-LIPOATES AND RELATED COMPOUNDSJ. Acta Pharmaceutica Sinica, 1984, 19(10): 742-747.
Citation: ZHOU Zhao-Wu, LIU Zhen-Gu, DAI Chang-Shi, MA Li-Ren. STUDIES ON ANTIRADIATION DRUG: SYNTHESIS OF AMINO-LIPOATES AND RELATED COMPOUNDSJ. Acta Pharmaceutica Sinica, 1984, 19(10): 742-747.

抗辐射药物的研究:硫辛酸氨基酯的合成

STUDIES ON ANTIRADIATION DRUG: SYNTHESIS OF AMINO-LIPOATES AND RELATED COMPOUNDS

  • 摘要: 本文报道35个硫辛酸氨基酯的合成和抗辐射作用。采刚四种不同方法进行酯的合成,对于一些中间体的合成方法也作了改进。硫辛酸氨基酯化合物中的环状双硫结构可能是其抗辐射作用的有效部分,而侧链则可以加以改变,在酯键的α-碳上引入β-肾上腺素能阻断剂或“双酯”结构后抗辐射作用非常显著,如化合物2,16,25,27等。化合物10对狗有明显升高外周血白细胞的作用。

     

    Abstract: Thirty-five amino-lipoates were synthesized and their antiradiation activity investigated. The polymerizable dithiolane ring possibly represents the main effective part, while the side chain the less effective part, as it may be altered to certain extent without losing antiradiation activity.Four different routes were described for synthesizing these amino-lipoates with satisfactory results. Improved methods for synthesizing the intermediates were also reported.Compounds no. 2, 4, 22, 24, 25, 27, 29, 30, 31, 34 and 35 when administered intraperitoneally before irradiation increased the survival of mice to 50~70%. Compounds no. 24 and 27 were found to be effective when administered orally before irradiation, increasing 40% of the survival. Compounds no. 19, 25, 27 and 30 when administered intraperitoneally after irradiation, increased 25~45% of the survival. All these data are statistically significant in comparison with the control. Compound no.10 increased the leucocyte count in the peripheral blood in dogs.

     

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