Synthesis of 6-substituted 1-phenylbenzazepines and their dopamine D(1) receptor activities
文献类型:期刊论文
作者 | Zhang, Jing1; Chen, Xuetao2; Yu, Leiping2; Zhen, Xuechu2; Zhang, Ao1![]() |
刊名 | BIOORGANIC & MEDICINAL CHEMISTRY
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出版日期 | 2008-11-01 |
卷号 | 16期号:21页码:9425-9431 |
关键词 | Dopamine receptor Serotonin receptor 1-Phenylbenzazepine SKF-38393 SKF-83959 |
ISSN号 | 0968-0896 |
DOI | 10.1016/j.bmc.2008.09.049 |
文献子类 | Article |
英文摘要 | A series of racemic 6-aryl substituted 1-phenylbenzazepines 7a-e, and 17a,b were prepared. All these compounds showed binding potencies compatible to or much higher than that of the prototypic (+/-)-SKF- 38393 ((+/-)-1) and (+/-)-SKF-83959 (3) for the D(1) receptor. Among analogs of (+/-)-SKF-38393, compounds 7b, 7c and 7e possess 10-, 2- and 7-fold enhancement in binding for the D(1) receptor, respectively. Lower but compatible potency to that of (+/-)-1 was observed for compounds 7a and 7d. The optimal 6-substituents (m-tolyl, and 2 '-naphthyl) were applied to the skeleton of (+/-)-SKF-83959 (3). The resulting compounds 17a, b displayed high affinity at the D(1) receptor, only slightly lower than that of (3). These two compounds also showed good binding at the D(2) receptor. (C) 2008 Elsevier Ltd. All rights reserved. |
WOS关键词 | CROSS-COUPLING REACTIONS ; CONVENIENT SYNTHESIS ; AGONISTS ; ANALOGS ; AGENTS |
资助项目 | Chinese National Science Foundation[30672517] ; Shanghai Commission of Science and Technology[07pj14104] ; Ministry of Science and Technology[2007AA022163] ; Chinese Academy of Sciences[00000000] ; Shanghai Institute of Materia Medica[00000000] |
WOS研究方向 | Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry |
语种 | 英语 |
WOS记录号 | WOS:000260134400004 |
出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
源URL | [http://119.78.100.183/handle/2S10ELR8/279444] ![]() |
专题 | 药理学第二研究室 |
通讯作者 | Zhen, Xuechu |
作者单位 | 1.Chinese Acad Sci, SOMCL, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China 2.Chinese Acad Sci, Neuropharmacol Lab, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China; |
推荐引用方式 GB/T 7714 | Zhang, Jing,Chen, Xuetao,Yu, Leiping,et al. Synthesis of 6-substituted 1-phenylbenzazepines and their dopamine D(1) receptor activities[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2008,16(21):9425-9431. |
APA | Zhang, Jing,Chen, Xuetao,Yu, Leiping,Zhen, Xuechu,&Zhang, Ao.(2008).Synthesis of 6-substituted 1-phenylbenzazepines and their dopamine D(1) receptor activities.BIOORGANIC & MEDICINAL CHEMISTRY,16(21),9425-9431. |
MLA | Zhang, Jing,et al."Synthesis of 6-substituted 1-phenylbenzazepines and their dopamine D(1) receptor activities".BIOORGANIC & MEDICINAL CHEMISTRY 16.21(2008):9425-9431. |
入库方式: OAI收割
来源:上海药物研究所
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