Aminobenzisoxazole compounds as agonists of alpha 7 nicotinic acetylcholine receptors: a patent evaluation (WO 2017027600)
文献类型：期刊论文
| 作者 | He, Yang; Shen, Jingshan
|
| 刊名 | EXPERT OPINION ON THERAPEUTIC PATENTS
 |
| 出版日期 | 2018 |
| 卷号 | 28期号:5页码:429-436 |
| 关键词 | Nicotinic receptors alpha 7 nAchR cognition agonists allosteric modulators |
| ISSN号 | 1354-3776 |
| DOI | 10.1080/13543776.2018.1455827 |
| 文献子类 | Article |
| 英文摘要 | Introduction: alpha 7 subtype nicotinic acetylcholine receptor (7 nAChR) ligands, that is, ligands that interact with the orthosteric or allosteric binding sites of alpha 7 nAChR, hold great potential for several therapeutic applications. Numerous compounds have been designed targeting alpha 7 nAChR but most of them cannot be used therapeutically for various reasons. Areas covered: The patent application describes a series of germinal substituted aminobenzisoxazole compounds as alpha 7 nAChR ligands. These compounds were claimed as potential therapeutics for treating and/or improving cognitive function. All of the (R)-stereoisomer presented high binding activities for alpha 7 nAChR and several compounds displayed excellent selectivity over 5-HT3R. Expert opinion: The privileged structure-derived modification via bioisosterism and scaffold hopping is an important approach for seeking novel alpha 7 nAChR ligands. The claimed germinal substituted aminobenzisoxazole derivatives with low tPSA values as well as low number of hydrogen bond donors and acceptors are supposed to have sufficient BBB penetration. Although there is a lack of essential biological data and the molecular mechanisms are not clear, these compounds stand for a new type of alpha 7 nAChR ligands and deserve further studies. |
| WOS关键词 | POSITIVE ALLOSTERIC MODULATORS ; ALZHEIMERS-DISEASE ; CLINICAL-TRIALS ; DRUG DISCOVERY ; SCHIZOPHRENIA ; PHARMACOKINETICS ; ENCENICLINE ; CANDIDATES ; COGNITION ; TARGETS |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000430500300006 |
| 出版者 | TAYLOR & FRANCIS LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/272316]  |
| 专题 | 药物化学研究室 |
| 通讯作者 | Shen, Jingshan |
| 作者单位 | Chinese Acad Sci, Shanghai Inst Mat Med, CAS Key Lab Receptor Res, Shanghai, Peoples R China |
| 推荐引用方式 GB/T 7714 | He, Yang,Shen, Jingshan. Aminobenzisoxazole compounds as agonists of alpha 7 nicotinic acetylcholine receptors: a patent evaluation (WO 2017027600)[J]. EXPERT OPINION ON THERAPEUTIC PATENTS,2018,28(5):429-436. |
| APA | He, Yang,&Shen, Jingshan.(2018).Aminobenzisoxazole compounds as agonists of alpha 7 nicotinic acetylcholine receptors: a patent evaluation (WO 2017027600).EXPERT OPINION ON THERAPEUTIC PATENTS,28(5),429-436. |
| MLA | He, Yang,et al."Aminobenzisoxazole compounds as agonists of alpha 7 nicotinic acetylcholine receptors: a patent evaluation (WO 2017027600)".EXPERT OPINION ON THERAPEUTIC PATENTS 28.5(2018):429-436. |
入库方式： OAI收割
来源：上海药物研究所
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