药学学报, 1962, 9(3): 162-166
引用本文:
白东鲁;嵇汝运. 血吸虫病化学治疗的研究 Ⅹ.带有噻吩和四氢噻吩环的若干酰胺[J]. 药学学报, 1962, 9(3): 162-166.
BAI DONG-LU KYI ZU-YOONG . CHEMOTHERAPEUTIC STUDIES ON SCHISTOSOMIASIS Ⅹ.SOME AMIDES DERIVED FROM THIOPHENE-2-CARBOXYLIC,THIOPHENE-2-SULPHONIC ACID AND TETRAHYDROTHIOPHENE-2,5-DICARBOXYLIC ACID[J]. Acta Pharmaceutica Sinica, 1962, 9(3): 162-166.

血吸虫病化学治疗的研究 Ⅹ.带有噻吩和四氢噻吩环的若干酰胺
白东鲁;嵇汝运
中国科学院药物研究所
摘要:
噻吩-2-甲酰氯及噻吩-2-磺酰氯分别与胺作用得相应的酰胺及磺酰胺。顺式四氢噻吩-2,5-二甲酸与氯化亚砜作用得到顺式四氢噻吩-2,5-二甲酰氯,后者与氨水及β-苯乙胺作用得到相应的二种酰胺,N,N′-双-(噻吩-2-甲酰基)-对-二氮六环用氢化锂铝还原,得到N,N′-双-(噻吩-2-甲基)-对-二氮六环。以上合成的化合物经动物试验均无疗效。
关键词:   
CHEMOTHERAPEUTIC STUDIES ON SCHISTOSOMIASIS Ⅹ.SOME AMIDES DERIVED FROM THIOPHENE-2-CARBOXYLIC,THIOPHENE-2-SULPHONIC ACID AND TETRAHYDROTHIOPHENE-2,5-DICARBOXYLIC ACID
BAI DONG-LU KYI ZU-YOONG
Abstract:
It has been discovered in our Institute that Cucurbitine (Ⅰ) is an effective inhibitor against Schistosoma japonicum. In order to find chemical analogues which are more powerful inhibiting agents, various amides of thiophene-2-carboxylic acid, thiophene-2-sulphonic acid and tetrahydrothiophene-2, 5-dicarboxylic acid have been prepared. But none of these compounds was active on animal test. Oxidation of thiophene-2-formaldehyde by means of silver oxide gave thiophene-2-formic acid. On treating thiophene-2-formyl chloride and thiophene-2-sulphonyl chloride with various amines, the corresponding amides were readily formed. Reduction of N, N'-bis-(thiophene-2-carbonyl) piperazine by means of lithium aluminium hydride gave N, N'-bis-(thiophene-2-methyl) piperazine. Cis-tetrahydrothiophene-2,5-dicarbonyl chloride was formed when cis-tetrahydrothiophene-2, 5-dicarboxylic acid was treated with thionyl chloride. Cis-tetrahydrothiophene-2, 5-dicarbonyl chloride on treatment with aqueous ammonia and β-phenylethylamine gave 2, 5-dicarbamyltetrahydrothiophene and N, N'-bis-(β-phenylethyl)-2, 5-dicarbamyltetrahydrothiophene respectively.
Key words:   
收稿日期:
相关功能
PDF(273KB) Free
打印本文
0
作者相关文章