新型2-(吡啶-2-基)-1H-苯并咪唑衍生物作为强效葡萄糖激酶激活剂的发现。
Discovery of novel 2-(pyridine-2-yl)-1H-benzimidazole derivatives as potent glucokinase activators.
作者信息
Ishikawa Makoto, Nonoshita Katsumasa, Ogino Yoshio, Nagae Yoshikazu, Tsukahara Daisuke, Hosaka Hideka, Maruki Hiroko, Ohyama Sumika, Yoshimoto Riki, Sasaki Kaori, Nagata Yasufumi, Eiki Jun-Ichi, Nishimura Teruyuki
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 Aug 1;19(15):4450-4. doi: 10.1016/j.bmcl.2009.05.038. Epub 2009 May 18.
The synthesis and structure-activity-relationships (SARs) of novel 2-(pyridine-2-yl)-1H-benzimidazole glucokinase activators are described. Systematic modification of benzimidazole lead 5a identified from a high-throughput screening led to the discovery of a potent and metabolically stable glucokinase activator 16p(R) with greater structural diversity from GKAs reported to date. The compound also demonstrated acute oral glucose lowering efficacy in rat OGTT model.
描述了新型2-(吡啶-2-基)-1H-苯并咪唑葡萄糖激酶激活剂的合成及构效关系（SARs）。对从高通量筛选中鉴定出的苯并咪唑先导化合物5a进行系统修饰，发现了一种强效且代谢稳定的葡萄糖激酶激活剂16p(R)，其结构多样性比迄今报道的葡萄糖激酶激活剂更高。该化合物在大鼠口服葡萄糖耐量试验（OGTT）模型中也显示出急性降血糖功效。
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