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灭蚴药物的化学——Ⅰ.几种酯类、酰胺类及氯代酚类的化学结构与灭蚴作用的关系
CHEMISTRY OF CERCARICIDAL AGENTS OF SCHISTOSOMA JAPONICUM——Ⅰ.THE RELATION BETWEEN THE CHEMICAL CONSTITUTION AND CERCARICIDAL ACTIVITY OF SEVERAL GROUPS OF ESTERS,AMIDES AND CHLORINATED PHENOLS
【摘要】 <正> 一、前言使用化学药物杀灭血吸虫尾蚴的研究,在国外进行得不多,历史也较短.所试验过的药物,大部分是驱避剂,其次是杀虫药物、杀恙螨剂及杀菌剂等.Nolan 氏等曾做过比较系统的研究,共试验了75种药物,浸渍衣服后防护作用以十二酰二乙胺与邻苯二甲酸二丁酯等较为满意。Ferguson 等及 Wright 氏等证明,邻苯二甲酸的二丁酯和二甲酯、苯
【Abstract】 This paper discusses the relation between the constitution of different chemicals and their cer- caricidal activity.The tested chemicals are chlorinated phenols,benzoic esters,substituted benzoic esters,halogenated acetic esters,thiocyanated acetic esters,2-furan carboxylic esters,lauric esters, ω-undecylenic esters,and different amides.It has been found that the cercaricidal activity is influenced by the followings: (1)Substitution on the methyl carbon of the acetic esters with halogen,thiocyanogen or phenoxy group increases the activity. (2)The increase of the number of carbon atoms of the aliphatic acid part of the esters seems to be beneficial to the activity. (3)By increasing the substitution of halogen on the phenol ring,the activity is enhanced. (4)Changing of the amides to esters results in increasing activity. (5)By introducing diethylamino group into the β-position of the ethyl group of the ethyl esters,the activity is increased. The last one has the most pronounced effect,for example,B-diethylaminoethyl laurate is effective at 1:100,000,000 dilution,which is nearly 1,000 times more effective than the bis-(2- hydroxy-3,5,6-trichloro-phenyl)-methane(hexachlorophene).
- 【文献出处】 药学学报 ,Acta Pharmaceutica Sinica , 编辑部邮箱 ,1960年06期
- 【被引频次】2
- 【下载频次】23