位置:成果数据库 > 期刊 > 期刊详情页
含嘧啶环的1,3,4-噁二唑Mannich碱的合成及生物活性
  • ISSN号:0251-0790
  • 期刊名称:《高等学校化学学报》
  • 时间:0
  • 分类:O626.27[理学—有机化学;理学—化学]
  • 作者机构:[1]西北大学化学研究所,西安710069, [2]西北大学化工学院,西安710069, [3]西北大学化学与材料学院,西安710069
  • 相关基金:国家自然科学基金(批准号:21073141,21373161)资助.
中文摘要:

以芳香酸为原料,通过酯化、肼解及环化反应制得中间体5-芳基取代-1,3,4-嗯二唑-2-硫酮(c1-C3),然后中间体与甲醛和取代氨基嘧啶(D1~D5)发生Mannich反应得到-系列新型含有嘧啶环的1,3,4-嗯二唑类衍生物(E1-E15).所得目标化合物的结构经元素分析、IR及1HNMR确认.初步的生物活性测定结果表明,大部分目标化合物对植物病原菌有很好的抑制作用,其中化合物E3和E8的抑菌效果优于对照药三唑酮.

英文摘要:

1,3,4-Oxadiazole derivatives were reported to possess a broad spectrum of biological activities, such as antifungal, antibacterial, antiviral and antitubercular. Mannich bases had also been reported as potential biological agents, they were applicated in the fields of synthetic study and medicinal chemistry. In recent years, Mannich bases containing 1,3,4-oxadiazole ring had attracted a lot of attention and many Mannich bases of 1,3,4-oxadiazole bearing heterocycle scaffold were reported to have special bioactivity. Nevertheless, literature revealed that there were no reports of a molecular scaffold that Mannich base of 1,3,4-oxadiazole bearing pyrimidine. Prompted by these observations, a series of 1,3,4-oxadiazole derivatives containing pyrimidine( E1-E15 ) was synthesized from 5-aryl-1,3,4-oxadiazole-2-thione ( C1--C3 ), formaldehyde and substituted aminopyrimidine ( D1--D5 ) by Mannich reaction. 5-Aryl-1,3,4-oxadiazole-2-thione derivatives (C1--C3) were prepared from aromatic acids as the starting material via esterification, hydrazinolysis and cy clization. The structures of all title compounds were confirmed by elemental analysis, IR, 1H NMR techniques. Furthermore, their biological activities to four vegetable pathogens containing Gibberll nicotiancola, Gibberlla saubinetii, Fusarium oxysporium f. sp. niveum, Pythium solani had been tested. The preliminary results indicated that most of the compounds exhibit relatively good fungicidal activities, especially compounds E3 and E8 showed better biological activity than triazolone.

同期刊论文项目
同项目期刊论文
期刊信息
  • 《高等学校化学学报》
  • 北大核心期刊(2011版)
  • 主管单位:中华人民共和国教育部
  • 主办单位:吉林大学 南开大学
  • 主编:周其凤
  • 地址:吉林大学南胡校区
  • 邮编:130012
  • 邮箱:cjcu@jlu.edu.cn
  • 电话:0431-88499216
  • 国际标准刊号:ISSN:0251-0790
  • 国内统一刊号:ISSN:22-1131/O6
  • 邮发代号:12-40
  • 获奖情况:
  • 首届及第二届国家期刊奖,连续两届“百种中国杰出学术期刊”,中国期刊方阵“双高”期刊
  • 国内外数据库收录:
  • 俄罗斯文摘杂志,美国化学文摘(网络版),荷兰文摘与引文数据库,美国工程索引,美国科学引文索引(扩展库),日本日本科学技术振兴机构数据库,中国中国科技核心期刊,中国北大核心期刊(2004版),中国北大核心期刊(2008版),中国北大核心期刊(2011版),中国北大核心期刊(2014版),英国英国皇家化学学会文摘,中国北大核心期刊(2000版)
  • 被引量:50676