Design of novel carbamate acetylcholinesterase inhibitors based on the multiple binding sites of acetylcholinesterase
文献类型：期刊论文
| 作者 | Zhao, Qianfei; Yang, Guoquan; Mei, Xiangdong; Yuan, Huizhu; Ning, Jun |
| 刊名 | JOURNAL OF PESTICIDE SCIENCE
 |
| 出版日期 | 2008 |
| 卷号 | 33期号:4页码:371-375 |
| 关键词 | Carbamate Insecticides Acetylcholinesterase Multiple Binding Sites Inhibitory Activity Structure-activity Relationship |
| 英文摘要 | This work describes the design, synthesis, AChE inhibitory activity, and structure-activity relationship of compounds related to a recently discovered series of AChE inhibitors: phthalimide alkyloxyphenyl N-methylcarbamates. The influence of structural variations on inhibitory potency was carefully investigated by modifying different alkyloxy chain lengths and positions between phthalimide and phenyl N-methylcarbamate. The biological properties of the series were investigated in some detail by considering their activity on isolated enzymes. All of the newly synthesized derivatives, when tested on isolated AChE from the brain of the housefly (Musca domestica), were more active than phenyl N-methylcarbamate. In particular, compound II displayed the best AChE inhibition (352-fold higher than phenyl N-methylcarbamate, and 29-fold higher than metolcarb). which suggested that the phthalimide group of II bound strongly to the residues lining the gorge, and phenyl N-methylcarbamate bound at the catalytic sites. (C) Pesticide Science Society of Japan |
| WOS记录号 | WOS:000262695100005 |
| 源URL | [http://ir.rcees.ac.cn/handle/311016/22347]  |
| 专题 | 生态环境研究中心_中国科学院环境生物技术重点实验室 |
| 推荐引用方式 GB/T 7714 | Zhao, Qianfei,Yang, Guoquan,Mei, Xiangdong,et al. Design of novel carbamate acetylcholinesterase inhibitors based on the multiple binding sites of acetylcholinesterase[J]. JOURNAL OF PESTICIDE SCIENCE,2008,33(4):371-375. |
| APA | Zhao, Qianfei,Yang, Guoquan,Mei, Xiangdong,Yuan, Huizhu,&Ning, Jun.(2008).Design of novel carbamate acetylcholinesterase inhibitors based on the multiple binding sites of acetylcholinesterase.JOURNAL OF PESTICIDE SCIENCE,33(4),371-375. |
| MLA | Zhao, Qianfei,et al."Design of novel carbamate acetylcholinesterase inhibitors based on the multiple binding sites of acetylcholinesterase".JOURNAL OF PESTICIDE SCIENCE 33.4(2008):371-375. |
入库方式： OAI收割
来源：生态环境研究中心
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