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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 | |
| 引用本文： | 惠新平,王勤,王芳,张自义,管作武.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[J].有机化学,2006,26(12):1704-1708. |
| 作者姓名： | 惠新平 王勤 王芳 张自义 管作武 |
| 作者单位： | 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 |
| 基金项目： | 国家自然科学基金(No.20021001)，甘肃省自然科学基金(No.3ZS051-A25-005)资助项目. |
| 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 |
| 关 键 词： | 头孢菌素 半合成 抗菌活性 离心薄层层析 |
| 收稿时间： | 2006-1-13 |
| 修稿时间： | 2006年1月11日 |
Semisynthesis and Antibacterial Activity of 7β-[2-(2-Aminothiazol-4-yl)-(Z)-2-methoxyiminoacetylamido]-3-heterothiomethylcephalosporins |
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| HUI Xin-Ping,WANG Qin,WANG Fang,ZHANG Zi-Yi,GUAN Zuo-Wu.Semisynthesis and Antibacterial Activity of 7β-[2-(2-Aminothiazol-4-yl)-(Z)-2-methoxyiminoacetylamido]-3-heterothiomethylcephalosporins[J].Chinese Journal of Organic Chemistry,2006,26(12):1704-1708. | |
| Authors: | HUI Xin-Ping WANG Qin WANG Fang ZHANG Zi-Yi GUAN Zuo-Wu |
| Institution: | a State Key Laboratory of Applied Organic Chemistry, College of Chemistry and Chemical Engineering, Lanzhou University, Lanzhou 730000;b. School of Life Sciences, Lanzhou University, Lanzhou 730000;c. Peking University Health Science Center, Beijing 100083 |
| Abstract: | New cephalosporin derivatives 5a～5j 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. |
| Keywords: | cephalosporin semisynthesis antibacterial activity centrifugal-TLC |
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