具有高代谢稳定性和化学稳定性的基于水杨酸酯-尿素的可溶性环氧化物水解酶抑制剂。
Salicylate-urea-based soluble epoxide hydrolase inhibitors with high metabolic and chemical stabilities.
作者信息
Kasagami Takeo, Kim In-Hae, Tsai Hsing-Ju, Nishi Kosuke, Hammock Bruce D, Morisseau Christophe
机构信息
Department of Entomology and University of California Davis Cancer Center, University of California, One Shields Avenue, Davis, CA 95616, USA.
出版信息
Bioorg Med Chem Lett. 2009 Mar 15;19(6):1784-9. doi: 10.1016/j.bmcl.2009.01.069. Epub 2009 Jan 27.
Abstract
We investigated N-adamantyl-N'-phenyl urea derivatives as simple sEH inhibitors. Salicylate ester derivatives have high inhibitory activities against human sEH, while the free benzoic acids are less active. The methyl salicylate derivative is a potent sEH inhibitor, which also has high metabolic and chemical stabilities; suggesting that such inhibitors are potential lead molecule for bioactive compounds acting in vivo.
摘要
我们研究了N-金刚烷基-N'-苯基脲衍生物作为简单的可溶性环氧化物水解酶（sEH）抑制剂。水杨酸酯衍生物对人sEH具有高抑制活性，而游离苯甲酸的活性较低。水杨酸甲酯衍生物是一种有效的sEH抑制剂，它还具有高代谢稳定性和化学稳定性；这表明此类抑制剂是体内生物活性化合物的潜在先导分子。
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