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新型缩氨基硫脲衍生物——氨基巯三唑Schiff碱的合成与抗菌活性
引用本文:侯宁,徐丽君. 新型缩氨基硫脲衍生物——氨基巯三唑Schiff碱的合成与抗菌活性[J]. 药学学报, 1992, 27(10): 738-742
作者姓名:侯宁  徐丽君
作者单位:山东医科大学药学系,济南250012;*山东省医药工业研究所,济南山大北路54号,邮政编码250100
摘    要:设计合成了新型缩氨基硫脲衍生物4-氨基-3-(呋喃-2)-5-巯基-1,2,4-三唑及其十种不同醛的Schiff碱衍生物,并进行了抑菌实验。结果表明:Schiff碱化合物结构中的甲亚胺基是该类化合物的活性功能基。苯环上更换不同的取代基对其活性有一定的影响,其中化合物4-(5-硝基亚糠基氨基)-3-(呋喃-2)-5-巯基-1,2,4-三唑(Ik)抗菌活性最高且抗菌谱最广;化合物4-亚水杨基氨基-3-(呋喃-2)-5-巯基-1,2,4-三唑(Ib)具有较强的抑霉活性。

关 键 词:缩氨基流脲  巯三唑  抑菌活性  抑霉活性
收稿时间:1991-10-31

SYNTHESIS AND BACTERIOSTATIC ACTIVITY OF NEW THIOSEMICARBAZONE DERIVATIVES-AMINO MERCAPTOTRIAZOLE SCHIFF BASES
N Hou,LJ Xu. SYNTHESIS AND BACTERIOSTATIC ACTIVITY OF NEW THIOSEMICARBAZONE DERIVATIVES-AMINO MERCAPTOTRIAZOLE SCHIFF BASES[J]. Acta pharmaceutica Sinica, 1992, 27(10): 738-742
Authors:N Hou  LJ Xu
Affiliation:Department of Pharmacy, Shandong Medical University, Jinan.
Abstract:4-amino-3-(furan-2)-5-mercapto-1,2,4-triazole (Ia) and its ten Schiff bases derived from Ia with different aldehydes were synthesized. All the compounds were screened for activity against seven bacteria and three fungi. Most compounds were found to possess different inhibition effect on some bacteria and fungi. The azomethine group of Schiff bases is the active functional group and the substituted groups on the phenyl ring had definite effect on the bacteriostatic and fungistatic activities. 4-(5-Nitrofurfurylideneamino)-3-(furan-2)-5-mercapto-1,2,4-tria zol e (Ik) showed the most powerful antibacterial activity and broad antibacterial spectrum, while 4-salicylideneamino-3-(furan-2)-5-mercapto-1,2,4-triazole possessed strong activity against fungi.
Keywords:Mercaptotriazoles  Antibacterial activities  Antifungal activities  Thiosemicarbazones
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