Synthesis and biological evaluation of novel marine-derived indole-based 1,2,4-oxadiazoles derivatives as multifunctional neuroprotective agents
文献类型：期刊论文
| 作者 | Jiang, Cheng-Shi1; Fu, Yan1; Zhang, Li1; Gong, Jing-Xu1; Wang, Zhen-Zhong2; Xiao, Wei2; Zhang, Hai-Yan1 ; Guo, Yue-Wei1
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| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
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| 出版日期 | 2015-01-15 |
| 卷号 | 25期号:2页码:216-220 |
| 关键词 | Phidianidines 1,2,4-Oxadiazole derivatives Amyloid-beta-peptide Oxygen-glucose deprivation Neuroprotective activity |
| ISSN号 | 0960-894X |
| DOI | 10.1016/j.bmcl.2014.11.068 |
| 文献子类 | Article |
| 英文摘要 | Phidianidines (1), isolated from the marine opisthobranch mollusk Phidiana militaris, present the first example of natural products possessing an 1,2,4-oxadiazole ring system and show various bioactivities. However, the structure-activity relationship study related to 1 has not been reported yet. As our ongoing effect toward marine-derived potential neuroprotective agents, a series of phidianidine-based derivatives have been synthesized and evaluated for neuroprotective effects against amyloid-beta(25-35) (A beta(25-35))-, hydrogenperoxide (H2O2)-, and oxygen-glucose deprivation (OGD)-induced neurotoxicity in SH-SY5Y cells. The bioassay results indicated that some of analogs, especially 2q and 2r, exhibited good in vitro neuroprotective effects in the above three screening models. The preliminary SAR study indicated that substituent groups introduced to the benzene ring play a crucial role in their bioactivity. In particular, the linear alkoxy group at 4-position favors the neuroprotective activity, while a bulky group could lead the activity decrease or loss. These findings could provide an alternative strategy for the development of novel indole-based 1,2,4-oxadiazole derivatives for the treatment of Alzheimer's disease. (C) 2014 Elsevier Ltd. All rights reserved. |
| WOS关键词 | NEURODEGENERATIVE DISEASES ; NATURAL-PRODUCTS ; CELL-DEATH ; PHIDIANIDINES ; ALKALOIDS |
| 资助项目 | National Marine '863' Projects[2013AA092902] ; Natural Science Foundation of China[81302692] ; Natural Science Foundation of China[81273430] ; STCSM Projects[14431901100] |
| WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000347901400012 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/276671]  |
| 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 天然药物化学研究室 |
| 通讯作者 | Xiao, Wei |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China; 2.Jiangsu Kanion Pharmaceut Co Ltd, Lianyungang 222001, Peoples R China |
| 推荐引用方式 GB/T 7714 | Jiang, Cheng-Shi,Fu, Yan,Zhang, Li,et al. Synthesis and biological evaluation of novel marine-derived indole-based 1,2,4-oxadiazoles derivatives as multifunctional neuroprotective agents[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2015,25(2):216-220. |
| APA | Jiang, Cheng-Shi.,Fu, Yan.,Zhang, Li.,Gong, Jing-Xu.,Wang, Zhen-Zhong.,...&Guo, Yue-Wei.(2015).Synthesis and biological evaluation of novel marine-derived indole-based 1,2,4-oxadiazoles derivatives as multifunctional neuroprotective agents.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,25(2),216-220. |
| MLA | Jiang, Cheng-Shi,et al."Synthesis and biological evaluation of novel marine-derived indole-based 1,2,4-oxadiazoles derivatives as multifunctional neuroprotective agents".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 25.2(2015):216-220. |
入库方式： OAI收割
来源：上海药物研究所
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