基本信息:
- 专利标题： 具有抗耐药菌活性的季铵查尔酮衍生物、其制备方法及应用
- 专利标题（英）：Quatemary ammonium chalcone derivatives resistant to drug-resistance bacteria activities, preparation method and application of quatemary ammonium chalcone derivatives
- 申请号：CN201710474526.7 申请日：2017-06-21
- 公开(公告)号：CN107235894A 公开(公告)日：2017-10-10
- 发明人： 张恩 , 秦上尚 , 楚文超 , 白鹏燕 , 杨兆青 , 崔得运 , 化永刚 , 王铭铭 , 王亚娜 , 刘宏民
- 申请人： 郑州大学
- 申请人地址： 河南省郑州市高新区科学大道100号
- 专利权人： 郑州大学
- 当前专利权人： 郑州大学
- 当前专利权人地址： 河南省郑州市高新区科学大道100号
- 代理机构： 郑州联科专利事务所
- 代理人： 时立新
- 主分类号： C07D213/50
- IPC分类号： C07D213/50 ; C07D213/61 ; C07D307/46 ; C07D333/22 ; C07C237/04 ; C07C231/12 ; A61P31/04
The invention belongs to the technical field of medicinal chemistry, and discloses quatemary ammonium chalcone derivatives resistant to drug-resistance bacteria activities, a preparation method and application of the quatemary ammonium chalcone derivatives. A structural formula is as shown in the description. Proved by invitro antibacterial activity experiments and erythrocyte hemolytic experiments, a large part of compounds in the series of the derivatives have great antibacterial effects and selections on staphylococcus aureus and colonic enterococcus faecalis of gram-positive bacteria, escherichia coli and pseudomonas aeruginosa of gram-negative bacteria. The selected part of compounds show great antimicrobial activities on a plurality of 'superbacteria' including methicillin-resistant staphylococcus aureus (MRSA), vancomycin resistant enterococcus (VRE), carbapenem-resistant enterobacteriaceae (CRE) and new delhi metallo (NDM) carrying NDM genes, and especially show excellent activities on the MRSA. Proved by invitro erythrocyte toxicity experiments, the series of compounds are low in erythrocyte toxicity and can be adopted as new anti-microbial drug candidates.
公开/授权文献:
- CN107235894B 具有抗耐药菌活性的季铵查尔酮衍生物、其制备方法及应用 公开/授权日：2020-04-03
IPC结构图谱:
| C | 化学；冶金 |
| --C07 | 有机化学 |
| ----C07D | 杂环化合物 |
| ------C07D213/00 | 杂环化合物，含六元环、不与其他环稠合、有1个氮原子作为仅有的杂环原子、环原子间或环原子与非环原子间有3个或更多个双键 |
| --------C07D213/02 | .环原子间或环原子与非环原子间有3个双键 |
| ----------C07D213/04 | ..在环氮原子与非环原子间没有键或只有氢或碳原子直接连在环氮原子上 |
| ------------C07D213/06 | ...除了环氮原子外，只含氢和碳原子 |
| --------------C07D213/28 | ....被以单键键合的氧原子或硫原子取代的基 |
| ----------------C07D213/46 | .....氧原子 |
| ------------------C07D213/50 | ......酮基 |