Discovery of novel 2,6-disubstituted pyridazinone derivatives as acetylcholinesterase inhibitors
文献类型：期刊论文
| 作者 | Xing, Weiqiang1; Fu, Yan2; Shi, Zhangxing1; Lu, Dong1; Zhang, Haiyan2 ; Hu, Youhong1
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| 刊名 | EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
 |
| 出版日期 | 2013-05 |
| 卷号 | 63页码:95-103 |
| 关键词 | Pyridazinone Acetylcholinesterase Alzheimer's disease Docking study |
| ISSN号 | 0223-5234 |
| DOI | 10.1016/j.ejmech.2013.01.056 |
| 文献子类 | Article |
| 英文摘要 | 2,6-Disubstituted pyridazinone 4 was identified by HTS as a novel acetylcholinesterase (AChE) inhibitor. Under SAR development, compound 17e stood out as displaying high AChE inhibitory activity and AChE/butyrylcholinesterase (BuChE) selectivity in vitro. Docking studies revealed that 17e might interact with the catalytic active site (CAS) and the peripheral anionic site (PAS) simultaneously. Based on this novel binding information, 6-ortho-tolylamino and N-ethyl-N-isopropylacetamide substituted piperidine were disclosed as new PAS and CAS binders. (c) 2013 Elsevier Masson SAS. All rights reserved. |
| WOS关键词 | BETA-AMYLOID AGGREGATION ; ALZHEIMERS-DISEASE SYNTHESIS ; HIGHLY POTENT ; BIOLOGICAL EVALUATION ; BERBERINE DERIVATIVES ; ACHE INHIBITORS ; TACRINE CONGENERS ; DUAL INHIBITORS ; HUPERZINE-B ; IN-VITRO |
| 资助项目 | National Science & Technology Major Project "Key New Drug Creation and Manufacturing Program"[2012ZX09301001-001] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000322855400010 |
| 出版者 | ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/277628]  |
| 专题 | 药理学第二研究室 中科院受体结构与功能重点实验室 新药研究国家重点实验室 药物化学研究室 |
| 通讯作者 | Zhang, Haiyan |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, Dept Med Chem, State Key Lab Drug Res, Shanghai 201203, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, Dept Neuropharmacol, State Key Lab Drug Res, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Xing, Weiqiang,Fu, Yan,Shi, Zhangxing,et al. Discovery of novel 2,6-disubstituted pyridazinone derivatives as acetylcholinesterase inhibitors[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2013,63:95-103. |
| APA | Xing, Weiqiang,Fu, Yan,Shi, Zhangxing,Lu, Dong,Zhang, Haiyan,&Hu, Youhong.(2013).Discovery of novel 2,6-disubstituted pyridazinone derivatives as acetylcholinesterase inhibitors.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,63,95-103. |
| MLA | Xing, Weiqiang,et al."Discovery of novel 2,6-disubstituted pyridazinone derivatives as acetylcholinesterase inhibitors".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 63(2013):95-103. |
入库方式： OAI收割
来源：上海药物研究所
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