首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Cyclization of some carbothioamide derivatives containing antipyrine and triazole moieties and investigation of their antimicrobial activities.
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Cyclization of some carbothioamide derivatives containing antipyrine and triazole moieties and investigation of their antimicrobial activities.

机译:一些含有反紫贮和三唑部分的碳氮基胺衍生物的环化以及对其抗菌活性的研究。

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摘要

Acetohydrazide derivative containing both antipyrine and triazole nuclei (5) was obtained starting from ethyl hydrazinecarboxylate derivative (2) and 4-aminoantipyrine (1) by three steps. The treatment of compound 5 with CS(2) afforded the conversion of hydrazide function into 5-mercapto-1,3,4-oxadiazole ring leading to the formation of 7. Then, 7 gave the product containing triazolotriazine moiety (9) by the reaction with hydrazine hydrate. The synthesis of the compounds incorporating the 1,3,4-thiadiazole (10a-c), 1,2,4-triazole (11a-c) or 1,3-thiazole (12, 13) nucleus as third heterocycle was performed by the acidic or basic treatment of compounds 6a-c which were obtained from the reaction of 5 with several isothiocyanates, or by the condensation of 6a with two different phenacyl bromides, respectively. The antimicrobial activity study revealed that all the compounds showed good activities except 3-5.
机译:从乙基肼羧酸甲酯衍生物(2)和4-氨基酰亚胺(1)开始,获得含有反紫红素和三唑核(5)的丙基酰肼衍生物。 用Cs(2)的化合物5的处理得到了酰肼函数转化为5-巯基-1,3,4-氧代唑环,导致形成7.然后,7给予含有三唑二嗪部分(9)的产物 与肼水合物反应。 含有1,3,4-噻二唑(10A-C),1,2,4-三唑(11A-C)或1,3-噻唑(12,13)核作为第三杂环的化合物的合成是第三杂环的 化合物6A-C的酸性或基本处理,其用几种异硫氰酸酯的反应得到,或通过分别用两种不同的异苯基溴化物的6A缩合。 抗微生物活性研究表明,除3-5外,所有化合物都显示出良好的活动。

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