| Literature DB >> 19540111 |
Makoto Ishikawa1, Katsumasa Nonoshita, Yoshio Ogino, Yoshikazu Nagae, Daisuke Tsukahara, Hideka Hosaka, Hiroko Maruki, Sumika Ohyama, Riki Yoshimoto, Kaori Sasaki, Yasufumi Nagata, Jun-Ichi Eiki, Teruyuki Nishimura.
Abstract
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.Entities:
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Year: 2009 PMID: 19540111 DOI: 10.1016/j.bmcl.2009.05.038
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN: 0960-894X Impact factor: 2.823