Synthesis, structure-activity relationships, and biological evaluation of a series of benzamides as potential multireceptor antipsychotics
文献类型：期刊论文
| 作者 | Yang, Feipu1; Jiang, Xiangrui1 ; Li, Jianfeng1; Wang, Yu1; Liu, Yongjian2; Bi, Minghao2; Wu, Chunhui2; Zhao, Qingjie1; Chen, Weiming2; Yin, Jingjing2
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| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
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| 出版日期 | 2016-07-01 |
| 卷号 | 26期号:13页码:3141-3147 |
| ISSN号 | 0960-894X |
| 关键词 | D-2 5-HT1A 5-HT2A PCP-induced hyperactivity Catalepsy |
| DOI | 10.1016/j.bmcl.2016.04.087 |
| 文献子类 | Article |
| 英文摘要 | In the present study, a series of benzamides, endowed with potent dopamine D-2, serotonin 5-HT1A and 5-HT2A receptors properties, was synthesized and evaluated as potential antipsychotics. Among them, 3-(4-(4-(6-fluorobenzo[d]isoxazol-3-yl)-piperidin-1-yl)butoxy)-N-methylbenzamide (21) and its fluoro-substituted analogue (22) held the best pharmacological binding profiles. They not only presented potent activities for D-2, 5-HT1A, and 5-HT2A receptors, but were also endowed with low activities for 5-HT2C, H-1 receptors and hERG channels, suggesting a low propensity of inducing weight gain and QT prolongation. In animal models, compounds 21 and 22 reduced phencyclidine-induced hyperactivity with a high threshold for catalepsy induction. It thus provides potential candidates for further preclinical studies. (C) 2016 Elsevier Ltd. All rights reserved. |
| WOS关键词 | MAJOR DEPRESSIVE DISORDER ; 5-HT1A RECEPTOR AGONIST ; INDUCED WEIGHT-GAIN ; PARKINSONS-DISEASE ; ATYPICAL ANTIPSYCHOTICS ; SCHIZOPHRENIA ; EFFICACY ; DRUG ; HYPERACTIVITY ; PHARMACOLOGY |
| 资助项目 | Chinese Ministry of National Science and Technology create significant new drugs, special major science and technology[2013ZX09507001] |
| WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| WOS记录号 | WOS:000377470600035 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/275979]  |
| 专题 | 药物化学研究室 |
| 通讯作者 | Wang, Zhen; He, Yang |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, CAS Key Lab Receptor Res, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China; 2.Topharman Shanghai Co Ltd, 1088 Chuansha Rd, Shanghai 201209, Peoples R China |
| 推荐引用方式 GB/T 7714 | Yang, Feipu,Jiang, Xiangrui,Li, Jianfeng,et al. Synthesis, structure-activity relationships, and biological evaluation of a series of benzamides as potential multireceptor antipsychotics[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2016,26(13):3141-3147. |
| APA | Yang, Feipu.,Jiang, Xiangrui.,Li, Jianfeng.,Wang, Yu.,Liu, Yongjian.,...&Shen, Jingshan.(2016).Synthesis, structure-activity relationships, and biological evaluation of a series of benzamides as potential multireceptor antipsychotics.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,26(13),3141-3147. |
| MLA | Yang, Feipu,et al."Synthesis, structure-activity relationships, and biological evaluation of a series of benzamides as potential multireceptor antipsychotics".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 26.13(2016):3141-3147. |
入库方式： OAI收割
来源：上海药物研究所
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