Discovery of Benzofuran Derivatives that Collaborate with Insulin-Like Growth Factor 1 (IGF-1) to Promote Neuroprotection

详细信息    查看全文

• 作者：Takeshi Wakabayashi ; Norihito Tokunaga ; Kazuyuki Tokumaru ; Taiichi Ohra ; Nobuyuki Koyama ; Satoru Hayashi ; Ryuji Yamada ; Mikio Shirasaki ; Yoshitaka Inui ; Tetsuya Tsukamoto
• 刊名：Journal of Medicinal Chemistry
• 出版年：2016
• 出版时间：May 26, 2016
• 年：2016
• 卷：59
• 期：10
• 页码：5109-5114
• 全文大小：329K
• 年卷期：0
• ISSN：1520-4804

文摘

A series of benzofuran derivatives with neuroprotective activity in collaboration with IGF-1 was discovered using a newly developed cell-based assay involving primary neural cells prepared from rat hippocampal and cerebral cortical tissues. A structure–activity relationship study identified compound 8 as exhibiting potent activity and brain penetrability. An in vitro pharmacological study demonstrated that although IGF-1 and 8 individually exhibited the neuroprotective effect, the latter acted in collaboration with IGF-1 to enhance neuroprotective activity.