期刊
NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY
卷 393, 期 12, 页码 2529-2542出版社
SPRINGER
DOI: 10.1007/s00210-020-01868-4
关键词
Stachydrine derivatives; Organic synthesis; Biological activities; Ischemic stroke; Neuroprotective agent
资金
- Zhufeng Scholar Program of the Ocean University of China [841412016]
- Major Projects of Independent Innovation of Qingdao [15-4-13-zdzx-hy]
- Outstanding Talents Plan of Qingdao [15-10-3-15-(34)-zch]
- Aoshan Talents Training Program of Qingdao National Laboratory for Marine Science and Technology [2017ASTCP-OS08]
Stachydrine is a natural product with multiple protective biological activities, including those involved in preventing cancer, ischemia, and cardiovascular disease. However, its use has been limited by low bioavailability and unsatisfactory efficacy. To address this problem, a series of stachydrine derivatives (A1/A2/A3/A4/B1/B2/B3/B4) were designed and synthesized, and biological studies were carried out in vitro and in vivo. When compared with stachydrine, Compound B1 exhibited better neuroprotective effects in vitro, and significantly reduced infarction size in the model of the middle cerebral artery occlusion rat model. Therefore, Compound B1 was selected for further research on ischemic stroke.
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