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7β-[2-（2-氨噻唑-4-基）-（Z）-2-甲氧亚胺乙酰胺基]-3-杂环硫亚甲基头孢菌素衍生物的半合成及抗菌活性
  • ISSN号：0253-2786
  • 期刊名称：《有机化学》
  • 时间：0
  • 分类：O636.1[理学—高分子化学;理学—化学]
  • 作者机构：[1]兰州大学化学化工学院功能有机分子化学国家重点实验室,兰州730000, [2]兰州大学生命科学学院,兰州730000, [3]北京大学医学部,北京100083
  • 相关基金：国家自然科学基金（No.20021001）和甘肃省自然科学基金（No.3ZS051-A25-005）资助项目.
作者： 惠新平[1], 王勤[2], 王芳[2], 张自义[1], 管作武[3]
关键词： 头孢菌素, 半合成, 抗菌活性, 离心薄层层析, cephalosporin, semisynthesis, antibacterial activity, centrifugal-TLC
中文摘要：

通过5-取代-1，3，4-噁二唑-2-硫醇（2a～2h），5-芳胺基-1，3，4-噻二唑-2-硫醇（2i～2j）和头孢菌素母体7-氨基头孢烷酸（7-ACA）反应，制得头孢菌素中间体3a～3j，用氨噻唑肟活性酯4和头孢菌素中间体缩合，合成了头孢菌素衍生物5a～5j．体外抗菌结果表明头孢菌素衍生物对革兰氏阳性菌和阴性菌均有显著抑制活性，对金黄色葡萄球菌尤为敏感．

英文摘要：

New cephalosporin derivatives 5a～Sj were prepared by condensation of 3a～3j with aminothiazoleoxime active ester 4. The intermediates 3a～3j were synthesized by the reaction of 5-substituted-1,3,4-oxadiazole-2-thiols （2a～2h）, 5-arylamino-1,3,4-thiadiazole-2-thiols （2i～2j） with 7-aminocephalosporanic acid （7-ACA）, respectively. The preliminary results of antibacterial activities revealed that compounds 5 showed obviously antibacterial activities against both Gram-positive and Gram-negative bacteria.

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期刊信息
  • 《有机化学》
  • 中国科技核心期刊
  • 主管单位:
  • 主办单位:中国化学会 中国科学院上海有机化学研究所
  • 主编：陈庆云
  • 地址：上海市枫林路354号
  • 邮编：200032
  • 邮箱：bianji@mail.sioc.ac.cn
  • 电话：021-54925244
  • 国际标准刊号：ISSN：0253-2786
  • 国内统一刊号：ISSN：31-1321/O6
  • 邮发代号:4-285
  • 获奖情况:
  • 中国期刊方阵“双效”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）,中国北大核心期刊（2000版）
  • 被引量:14408