新型强效2-氨基苯甲酰胺衍生物作为变构葡萄糖激酶激活剂的鉴定
Identification of novel and potent 2-amino benzamide derivatives as allosteric glucokinase activators.
作者信息
Nishimura Teruyuki, Iino Tomoharu, Mitsuya Morihiro, Bamba Makoto, Watanabe Hitomi, Tsukahara Daisuke, Kamata Kenji, Sasaki Kaori, Ohyama Sumika, Hosaka Hideka, Futamura Mayumi, Nagata Yasufumi, Eiki Jun-Ichi
机构信息
Banyu Tsukuba Research Institute, Banyu Pharmaceutical Co. Ltd., Okubo-3, Tsukuba, 300-2611 Ibaraki, Japan.
出版信息
Bioorg Med Chem Lett. 2009 Mar 1;19(5):1357-60. doi: 10.1016/j.bmcl.2009.01.053. Epub 2009 Jan 21.
The identification and structure-activity-relationships (SARs) of novel 2-amino benzamide glucokinase activators are described. Compounds in this series were developed to be potent GK activators, and their binding mode to the GK protein was determined by crystal structure analysis. In vivo pharmacokinetic and acute in vivo efficacy studies of compound 18 are also described.
本文描述了新型2-氨基苯甲酰胺葡萄糖激酶激活剂的鉴定及其构效关系（SARs）。该系列化合物被开发为强效的GK激活剂，并通过晶体结构分析确定了它们与GK蛋白的结合模式。文中还介绍了化合物18的体内药代动力学和急性体内疗效研究。
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