Synthesis and biological evaluation of a series of multi-target N-substituted cyclic imide derivatives with potential antipsychotic effect
文献类型：期刊论文
| 作者 | Xu, Mingshuo2,3; Wang, Yu2; Yang, Feipu2; Wu, Chunhui1; Wang, Zhen2 ; Ye, Bin1; Jiang, Xiangrui2; Zhao, Qingjie2; Li, Jianfeng2; Liu, Yongjian1
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| 刊名 | EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
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| 出版日期 | 2018-02-10 |
| 卷号 | 145页码:74-85 |
| 关键词 | Antipsychotic Cyclic imide Multi-target 5-HT1A receptor |
| ISSN号 | 0223-5234 |
| DOI | 10.1016/j.ejmech.2017.12.099 |
| 文献子类 | Article |
| 英文摘要 | In the present study, a series of multi-target N-substituted cyclic imide derivatives which possessed potent dopamine D2, serotonin 5-HT1A and 5-HT2A receptors properties were synthesized and evaluated as potential antipsychotics. Among these compounds, (3aR,4R,7S,7aS)-2-(4-(4-(benzo[b]thiophen-4-yl) piperazin-1-yl)butyl)-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindole-1,3(2H)-dione hydrochloride (3d) held a promising pharmacological profile. 3d not only showed potent and balanced in vitro activities on D-2/5-HT1A/5-HT2A receptors, but also endowed with low to moderate activities on 5-HT2c, H-1,H- alpha(1A), M-3 receptors and hERG channel, suggesting a low liability to induce side effects such as weight gain, orthostatic hypotension and QT prolongation. In animal behavioral studies, 3d reduced phencyclidine induced hyperlocomotion with a high threshold for catalepsy induction. Compound 3d was selected as a potential antipsychotic candidate for further development. (C) 2018 Elsevier Masson SAS. All rights reserved. |
| WOS关键词 | 5-HT1A RECEPTORS ; ATYPICAL ANTIPSYCHOTICS ; SEROTONIN RECEPTORS ; DRUG ACTION ; SCHIZOPHRENIA ; DISORDERS ; COGNITION ; AGONISTS ; METAANALYSIS ; MODELS |
| 资助项目 | Special Foundation of Chinese Academy of Sciences for strategic pilot technology[XDA12040208] ; R&D Program of Shanghai Municipal Science and Technology Commission[14431905500] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000425198200008 |
| 出版者 | ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/279904]  |
| 专题 | 药物化学研究室 |
| 通讯作者 | He, Yang; Shen, Jingshan |
| 作者单位 | 1.Topharman Shanghai Co Ltd, 1088 Chuansha Rd, Shanghai 201209, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Mat Med, CAS Key Lab Receptor Res, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China; 3.Univ Chinese Acad Sci, 19A Yuquan Rd, Beijing 100049, Peoples R China; |
| 推荐引用方式 GB/T 7714 | Xu, Mingshuo,Wang, Yu,Yang, Feipu,et al. Synthesis and biological evaluation of a series of multi-target N-substituted cyclic imide derivatives with potential antipsychotic effect[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2018,145:74-85. |
| APA | Xu, Mingshuo.,Wang, Yu.,Yang, Feipu.,Wu, Chunhui.,Wang, Zhen.,...&Jiang, Hualiang.(2018).Synthesis and biological evaluation of a series of multi-target N-substituted cyclic imide derivatives with potential antipsychotic effect.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,145,74-85. |
| MLA | Xu, Mingshuo,et al."Synthesis and biological evaluation of a series of multi-target N-substituted cyclic imide derivatives with potential antipsychotic effect".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 145(2018):74-85. |
入库方式： OAI收割
来源：上海药物研究所
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