Novel acetylcholinesterase inhibitors: Synthesis and structure-activity relationships of phthalimide alkyloxyphenyl N,N-dimethylcarbamate derivatives
文献类型：期刊论文
| 作者 | Zhao, Qianfei; Yang, Guoquan; Mei, Xiangdong; Yuan, Huizhu; Ning, Jun |
| 刊名 | PESTICIDE BIOCHEMISTRY AND PHYSIOLOGY
 |
| 出版日期 | 2009-11 |
| 卷号 | 95期号:3页码:131-134 |
| 关键词 | Carbamate insecticides AChE Multiple binding sites Phthalimide alkyloxyphenyl N Inhibitory activity Structure-activity relationship N-dimethylcarbamate |
| 中文摘要 | Based on the multiple binding sites of acetylcholinesterase (ACNE), a series of ACNE inhibitors: phthalimide alkyloxyphenyl N,N-dimethylcarbamate were designed and synthesized. ACNE inhibitory activity and structure-activity relationship of the compounds were researched also. The influence of structural variations on the inhibitory potency was carefully investigated by modifying different alkyloxy chain length and position between phthalimide and phenyl N,N-dimethylcarbamate (PDM). The biological properties of the series were investigated by considering the activity on isolated enzyme. Some of the newly synthesized derivatives, when tested on isolated ACNE from head of housefly (Musca domestica), were more active than PDM. The compounds J1, J2 and K1-K8 demonstrated higher inhibitory activity (5- to 404-fold) for ACNE than that of PDM. In particular, compound K1 displayed the best ACNE inhibition (404-fold higher than PDM), which suggested that phthalimide group of K1 strongly bound at the residues lining the gorge while phenyl N,N-dimethylcarbamate bound at the catalytic site. (C) 2009 Elsevier Inc. All rights reserved. |
| WOS记录号 | WOS:000270801200005 |
| 源URL | [http://ir.rcees.ac.cn/handle/311016/21541]  |
| 专题 | 生态环境研究中心_环境化学与生态毒理学国家重点实验室 |
| 推荐引用方式 GB/T 7714 | Zhao, Qianfei,Yang, Guoquan,Mei, Xiangdong,et al. Novel acetylcholinesterase inhibitors: Synthesis and structure-activity relationships of phthalimide alkyloxyphenyl N,N-dimethylcarbamate derivatives[J]. PESTICIDE BIOCHEMISTRY AND PHYSIOLOGY,2009,95(3):131-134. |
| APA | Zhao, Qianfei,Yang, Guoquan,Mei, Xiangdong,Yuan, Huizhu,&Ning, Jun.(2009).Novel acetylcholinesterase inhibitors: Synthesis and structure-activity relationships of phthalimide alkyloxyphenyl N,N-dimethylcarbamate derivatives.PESTICIDE BIOCHEMISTRY AND PHYSIOLOGY,95(3),131-134. |
| MLA | Zhao, Qianfei,et al."Novel acetylcholinesterase inhibitors: Synthesis and structure-activity relationships of phthalimide alkyloxyphenyl N,N-dimethylcarbamate derivatives".PESTICIDE BIOCHEMISTRY AND PHYSIOLOGY 95.3(2009):131-134. |
入库方式： OAI收割
来源：生态环境研究中心
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