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化学学报
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化学学报 ›› 1956, Vol. 22 ›› Issue (6): 566-571. 上一篇    下一篇

论文

异菸酰肼的N-氯乙酰衍生物及2, 6-二氨基异菸酸衍生物的合成及其抗结核作用

高怡生, 翁尊尧, 陆顺兴   

  1. 中国科学院药物研究所
  • 投稿日期:1956-09-12 发布日期:2013-06-03

THE PREPARATION AND THE ANTI-TUBERCULOSTATIC ACTION OF CHLOROACETYL DERIVATIVES OF ISONICOTINOYLHYDRAZINE AND DERIVATIVES OF 2, 6-DIAMINO-ISO-NICOTINIC ACID

KAO YEE-SHENG, OWEN TSUNG-YAO, LOH SHUEN-HSING   

  1. Institute of Materia Medica, Academia Sinica
  • Received:1956-09-12 Published:2013-06-03

PDF

700

被引次数

3

1.合成了三种异烟酰肼的衍生物,即sym-二氯乙酰基-异烟醯基肼、sym-三氯乙酰基-异烟酰基肼及sym-一氯乙酰基-异烟酰肼盐酸菾菜碱。这三种衍生物对B.sme-gmatis的抗菌作用分别为1:16,000;1:8,000;1:8,000。2.制备了八种2,6-二氨基异烟酸酯,即甲酯、乙酯、正丙酯、异丙酯、正丁酯、异丁酯、正戊酯、异戊酯。其中甲酯为已知物,馀为新化合物。其抗B.smegmatis的作用均为1:2000。3.2,6-二氨基-异烟酰肼的抗B.smegmatis为1:2000;2,6-二氨基-异烟酰胺及2,6-二氨基-异烟酸均无抗B.smegmatis作用。

The preparation of two derivatives of iso-nicotinoylhydrazine, namely, sym-dichloro-acetyl-iso-nicotinoylhydrazine and sym-trichloroacetyl-iso-nicotinoylhydrazine, has been described; and their inhibitory action against B, smegmatis was found to be at dilution of 1:16,000 and 1:8,000 respectively. The reaction between INH and monochloroacetyl chloride, however, led to the formation of a betaine hydrochloride of sym-chloroacetyl-iso-nicotinoylhydrazine, possessing also inhibitory action against the same organism at dilution of 1:8,000.