Literature DB >> 19540111

Discovery of novel 2-(pyridine-2-yl)-1H-benzimidazole derivatives as potent glucokinase activators.

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.

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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


  4 in total

1.  The use of docking-based comparative intermolecular contacts analysis to identify optimal docking conditions within glucokinase and to discover of new GK activators.

Authors:  Mutasem O Taha; Maha Habash; Mohammad A Khanfar
Journal:  J Comput Aided Mol Des       Date:  2014-03-08       Impact factor: 3.686

Review 2.  Management of type 2 diabetes: evolving strategies for the treatment of patients with type 2 diabetes.

Authors:  Ebenezer A Nyenwe; Terri W Jerkins; Guillermo E Umpierrez; Abbas E Kitabchi
Journal:  Metabolism       Date:  2011-01       Impact factor: 8.694

3.  Investigation of phytoconstituents of Enicostemma littorale as potential glucokinase activators through molecular docking for the treatment of type 2 diabetes mellitus.

Authors:  Altaf Khan; Aziz Unnisa; Mo Sohel; Mohan Date; Nayan Panpaliya; Shweta G Saboo; Falak Siddiqui; Sharuk Khan
Journal:  In Silico Pharmacol       Date:  2021-12-02

4.  New Triazinoindole Bearing Benzimidazole/Benzoxazole Hybrids Analogs as Potent Inhibitors of Urease: Synthesis, In Vitro Analysis and Molecular Docking Studies.

Authors:  Sundas Mumtaz; Shahid Iqbal; Mazloom Shah; Rafaqat Hussain; Fazal Rahim; Wajid Rehman; Shoaib Khan; Obaid-Ur-Rahman Abid; Liaqat Rasheed; Ayed A Dera; Hanan A Al-Ghulikah; Sana Kehili; Eslam B Elkaeed; Hamad Alrbyawi; Mohammed Issa Alahmdi
Journal:  Molecules       Date:  2022-10-04       Impact factor: 4.927

  4 in total

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