Synthesis and biological evaluation of a series of novel pyridinecarboxamides as potential multi-receptor antipsychotic drugs
文献类型：期刊论文
| 作者 | Xu, Mingshuo2,3; Wang, Yu3; Yang, Feipu3; Wu, Chunhui1; Wang, Zhen3 ; Ye, Bin1; Jiang, Xiangrui3; Zhao, Qingjie3; Li, Jianfeng3; Liu, Yongjian1
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| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
 |
| 出版日期 | 2018-02-15 |
| 卷号 | 28期号:4页码:606-611 |
| 关键词 | Antipsychotic Multi-receptor Pyridinecarboxamide 5-HT1A receptor PCP-induced hyperlocomotion |
| ISSN号 | 0960-894X |
| DOI | 10.1016/j.bmcl.2018.01.038 |
| 文献子类 | Article |
| 英文摘要 | In previous study, a series of benzamides was identified as potent antipsychotic agents. As a continuation of the program to discover novel antipsychotics, herein we reported the evaluation of a series of pyridinecarboxamide derivatives. The most promising compound 7h not only held good activities on dopamine D-2, serotonin 5-HT1A and 5-HT2A receptors, but also exhibited low potency for alpha(1A), H-1 and 5-HT2C receptors, indicating a low propensity of side effects like orthostatic hypotension and weight gain. Furthermore, 7h exhibited more potent antipsychotic-like effect than aripiprazole in behavioral studies. The preliminary results were promising enough for further research around this scaffold. (C) 2018 Elsevier Ltd. All rights reserved. |
| WOS关键词 | SEROTONIN RECEPTORS ; INDUCED CATALEPSY ; SCHIZOPHRENIA ; MECHANISM |
| 资助项目 | Special Fund for Strategic Pilot Technology of Chinese Academy of Sciences[XDA12040208] |
| WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000425882800012 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/279898]  |
| 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.Univ Chinese Acad Sci, 19A Yuquan Rd, Beijing 100049, Peoples R China; 3.Chinese Acad Sci, Shanghai Inst Mat Med, CAS Key Lab Receptor Res, 555 Zuchongzhi Rd, Shanghai 201203, 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 novel pyridinecarboxamides as potential multi-receptor antipsychotic drugs[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2018,28(4):606-611. |
| APA | Xu, Mingshuo.,Wang, Yu.,Yang, Feipu.,Wu, Chunhui.,Wang, Zhen.,...&Jiang, Hualiang.(2018).Synthesis and biological evaluation of a series of novel pyridinecarboxamides as potential multi-receptor antipsychotic drugs.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,28(4),606-611. |
| MLA | Xu, Mingshuo,et al."Synthesis and biological evaluation of a series of novel pyridinecarboxamides as potential multi-receptor antipsychotic drugs".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 28.4(2018):606-611. |
入库方式： OAI收割
来源：上海药物研究所
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