摘要
4-氨基-3-苯基-5-巯基-均-三唑(1)在无水乙酸钠作用下与β-氯苯丙酮(2)缩合得氨基三唑硫基苯丙酮(3)。化合物3与盐酸羟胺肟化得羰基肟化物(4),采用氯甲基噁二唑(5)对化合物4的肟羟基醚化得均三唑席夫碱噁二唑肟醚(6a^6e)。肟化物6a^6e与水杨醛缩合得到目标物席夫碱7a^7e。初步的体外抗菌实验表明,席夫碱肟醚类化合物7a^7e的活性明显高于氨基肟醚类化合物6a^6e,且对革兰氏阳性(Sa)的活性高于对革兰氏阴性菌(Ec)的。
The reaction of 4-amino-3-phenyl-5-mercapto-s-triazole （ 1 ） with β-chloro-phenyl-propanone （ 2 ） under refluxing ethanol in the presence of sodium acetate gave amino-triazolyl sulfanyl-phenylpropanone （3）. The oximation of compound 3 with hydroxyamine hydrochloride yielded the corresponding oxime （4） followed by the etherification with each of chloromethy-oxadiazoles （5a - 5e） and the condensation with salicylaldehyde to form oxime-ethers （6a - 6e） and schiff-base oxime-ethers （7a - 7e）, respectively. The antibacterial activities of the compounds synthesized in vitro to Gram positive bacteria and Gram negative bacteria were tested with the standard 2-fold agar dilution method, and all the tested compounds exhibited relatively better activities against Gram positive bacteria than those against Gram negative bacteria.
出处
《应用化学》
CAS
CSCD
北大核心
2007年第3期310-313,共4页
Chinese Journal of Applied Chemistry
基金
河南大学重点科研基金资助项目(04ZDZR009)
关键词
均-三唑
噁二唑
肟醚
席夫碱
合成
抗菌活性
s-triazole, oxadiazole, omixe-ether, Schiff-base, synthesis, antibacterial activity
