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咪唑并[1,5-a]吡嗪衍生物作为急性缺血性中风治疗药物的合成及其对c-Src的抑制活性

Synthesis and c-Src inhibitory activity of imidazo[1,5-a]pyrazine derivatives as an agent for treatment of acute ischemic stroke.

作者信息

Mukaiyama Harunobu, Nishimura Toshihiro, Kobayashi Satoko, Ozawa Tomonaga, Kamada Noboru, Komatsu Yoshimitsu, Kikuchi Shinji, Oonota Hideki, Kusama Hiroshi

机构信息

Central Research Laboratory, Kissei Pharmaceutical Company Ltd, 4365-1, Azumino-city, Nagano 399-8304, Japan.

出版信息

Bioorg Med Chem. 2007 Jan 15;15(2):868-85. doi: 10.1016/j.bmc.2006.10.041. Epub 2006 Oct 24.

DOI:10.1016/j.bmc.2006.10.041
PMID:17095233
Abstract

We synthesized and evaluated a series of C-5 substituted imidazo[1,5-a]pyrazine derivatives to identify potent c-Src inhibitors as potential therapeutic agents for acute ischemic stroke. Among these compounds, compound 14c.HCl demonstrated remarkable central nervous system (CNS) penetration and significant neuroprotective efficacy in vivo in rat models.

摘要

我们合成并评估了一系列C-5取代的咪唑并[1,5-a]吡嗪衍生物，以确定强效的c-Src抑制剂作为急性缺血性中风的潜在治疗药物。在这些化合物中，化合物14c.HCl在大鼠模型中显示出显著的中枢神经系统（CNS）渗透性和体内显著的神经保护功效。

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