Abstract

New series of bis(amino-1,2,4-triazoles ‏) 5a–f were prepared by the reaction of bis(chloro) diamides 3a–d with 5-substituted-4-amino-1,2,4-triazoles-3-thiole (4a–c). Reaction of bis(amino) triazoles 5a–d with the appropriate aldehydes afforded the corresponding Schiff bases 7a–d in good yields. Similarly, cyclocondansation of bis(amino) triazoles 5a–d with 1,3-bis(2-formyphenoxy)-2-propanol furnished the desired lariat macrocycles 12a–d. The antimicrobial activities of the prepared bis(amines) 5a–c, e–g, Schiff bases 7a–d, 11a–b and lariat macrocycles 12a,c,d were evaluated against series of selected microorganisms. Some of the prepared derivatives showed good antimicrobial activity against gram positive bacteria and gram negative bacteria. The MIC values for some of the tested compound were investigated.

摘要

通过双（氯）二酰胺3a-d与 5-取代的-4-氨基-1,2,4-三唑-反应制备新系列双（氨基-1,2,4-三唑‏）5a-f 3-硫醇（4a-c）。双（氨基）三唑5a-d与适当的醛反应以良好的收率提供相应的席夫碱7a-d。类似地，双（氨基）三唑5a-d与 1,3-双（2-甲酰苯氧基）-2-丙醇的环缩合反应提供了所需的套索大环12a-d。制备的双（胺）5a-c、e-g、席夫碱7a-d、11a-b和套索大环12a、c、d的抗菌活性针对一系列选定的微生物进行了评估。一些制备的衍生物对革兰氏阳性菌和革兰氏阴性菌表现出良好的抗菌活性。研究了一些测试化合物的 MIC 值。