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一些新型含氟三唑并噻二嗪作为潜在抗菌、抗真菌和抗癌药物的合成与研究。

Synthesis and studies on some new fluorine containing triazolothiadiazines as possible antibacterial, antifungal and anticancer agents.

作者信息

Shivarama Holla B, Sooryanarayana Rao B, Sarojini B K, Akberali P M, Suchetha Kumari N

机构信息

Department of Post-Graduate Studies and Research in Chemistry, Mangalore University, Mangalagangothri 574 199, India.

出版信息

Eur J Med Chem. 2006 May;41(5):657-63. doi: 10.1016/j.ejmech.2006.02.001. Epub 2006 Apr 17.

Abstract

Synthesis of a series of 7-arylidene-6-(2,4-dichlorophenyl)-3-aryloxymethyl/anilinomethyl-1,2,4-triazolo[3,4-b]-1,3,4-thiadiazines (3) by the condensation of 3-aryl-1-(2,4-dichloro-5-fluorophenyl)-2-bromo-propen-1-one (1) and 4-amino-5-mercapto-3-aryloxymethyl/anilinomethyl-1,2,4-triazoles (2) is described. The newly synthesized compounds were characterized by elemental analysis IR, 1H NMR and mass spectral data. These compounds were tested for their antimicrobial activities against Escherichia coli, Staphylococcus aureus (Smith), Psuedomonas aeruginosa (Gessard), Bacillus subtilis and Candida albicans. Some of the newly synthesized compounds were also screened for their anticancer activity. Among them compounds 3m, 3o, 3q showed in vitro anticancer activity.

摘要

通过3-芳基-1-(2,4-二氯-5-氟苯基)-2-溴-丙烯-1-酮(1)与4-氨基-5-巯基-3-芳氧基甲基/苯胺甲基-1,2,4-三唑(2)缩合反应合成了一系列7-亚芳基-6-(2,4-二氯苯基)-3-芳氧基甲基/苯胺甲基-1,2,4-三唑并[3,4-b]-1,3,4-噻二嗪(3)。通过元素分析、红外光谱、1H核磁共振和质谱数据对新合成的化合物进行了表征。测试了这些化合物对大肠杆菌、金黄色葡萄球菌(史密斯株)、铜绿假单胞菌(热萨德株)、枯草芽孢杆菌和白色念珠菌的抗菌活性。还对一些新合成的化合物进行了抗癌活性筛选。其中化合物3m、3o、3q表现出体外抗癌活性。

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