噻吩酮、醛缩氨硫脲衍生物的合成  

SYNTHESIS OF 2-ACETYLTHIOPHENE THIOSEMICARBAZONE DERIVATIVES

作　　者：王锐[1] 顾旭初 靳立人[1] 杨洁[2] 吴立云[2] 张岗[2] 吴秀琴[1] 冷宗康[1] 

机构地区：[1]南京药物研究所,210009 [2]中国药科大学

出　　处：《中国药科大学学报》1990年第1期6-10,共5页Journal of China Pharmaceutical University

摘　　要：采用A,B两法合成2-乙酰噻吩缩氨硫脲、2-甲酰噻吩缩氨硫脲(Ⅴ)及3-取代-4-氧噻唑烷-2叉-(2′-乙酰噻吩)腙(Ⅵ)等化合物,计31个。A法:以肼基二硫代羧酸甲酯与乙酰噻吩或噻吩醛缩合,再与各种胺反应制得化合物Ⅴ。B法:N^4取代的氨基硫脲中间体,与乙酰噻吩或噻吩醛缩合得化合物Ⅴ,再与氯乙酸环合而成化合物Ⅵ。对上述化合物进行伯氏鼠疟的抑制性治疗作用和约氏鼠疟的病因性予防作用筛选,未发现有明显的抗疟活性。对其中13个化合物及两个中间体进行体外抑菌试验,中间体3-[1-(2-噻吩)甲叉]肼基二硫代酸甲酯(Ⅳ_2)对革兰氏阳性菌有较好的抑制作用,对革兰氏阴性菌仅有中度以上的敏感性。In order to search for a potential antimalarial, 31 compounds of 2-acetylthiophene thiosemicarbazones (or 2-formylthiophene thiosemicarbazones) [Ⅴ] and 3-substituted-4-oxo-thiazolidine-2-ylidene(2′-acetylthiophene) hydrazones [Ⅵ] were prepared. The tests to examine the activities in mice were conducted, according to P. berghei and P. yoelii. None of these compounds had any significant activity. On the other hand, 13 compounds of 2-acetylthiophene thiosemicarbazones and 2 intermediates were tested for antibacterial activities. The results showed the intermediate [methyl 3- (1- (2- thiophene) methylen) hydrazinecarbodithioates] possessed antibacterial activity.

关 键 词：噻吩缩氨硫脲 合成 抗菌活性 

分 类 号：TQ463.53[化学工程—制药化工]