Imidazole derivatives as new potent and selective 20-HETE synthase inhibitors

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• 作者：Nakamura ; Toshio ; Kakinuma ; Hiroyuki ; Umemiya ; Hiroki ; Amada ; Hideaki ; Miyata ; Noriyuki ; Taniguchi ; Kazuo ; et. al.
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2004
• 出版时间：January, 2004
• 年：2004
• 卷：14
• 期：2
• 页码：333-336
• 全文大小：166 K

文摘

In a previous paper, we reported that an imidazole derivative 1 exhibited a potent inhibitory activity of 20-HETE synthase (1; IC₅₀ value of 5.7 nM), but this compound also exhibited little selectivity for cytochrome P450s (CYPs). We examined some derivatives of imidazole 1 which had an amino group on the side chain, and found that a dimethylaminohexyloxy derivative (3g; IC₅₀ value of 8.8 nM) showed potent and selective inhibitory activity.