Literature DB >> 19362831

Discovery of novel 3,6-disubstituted 2-pyridinecarboxamide derivatives as GK activators.

Morihiro Mitsuya1, Kenji Kamata, Makoto Bamba, Hitomi Watanabe, Yasuhiro Sasaki, Kaori Sasaki, Sumika Ohyama, Hideka Hosaka, Yasufumi Nagata, Jun-ichi Eiki, Teruyuki Nishimura.   

Abstract

A novel class of 3,6-disubstituted 2-pyridinecarboxamide derivatives was designed based on X-ray analysis of the 2-aminobenzamide lead class. Subsequent chemical modification led to the discovery of potent GK activators which eliminate potential toxicity concerns associated with an aniline group of the lead structure. Compound 7 demonstrated glucose lowering effect in a rat OGTT model.

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Year:  2009        PMID: 19362831     DOI: 10.1016/j.bmcl.2009.03.137

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  6 in total

1.  Design and Synthesis of Acetylenyl Benzamide Derivatives as Novel Glucokinase Activators for the Treatment of T2DM.

Authors:  Kaapjoo Park; Byoung Moon Lee; Kwan Hoon Hyun; Taedong Han; Dong Hoon Lee; Hyun Ho Choi
Journal:  ACS Med Chem Lett       Date:  2015-01-14       Impact factor: 4.345

2.  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

3.  Strain analysis of protein structures and low dimensionality of mechanical allosteric couplings.

Authors:  Michael R Mitchell; Tsvi Tlusty; Stanislas Leibler
Journal:  Proc Natl Acad Sci U S A       Date:  2016-09-21       Impact factor: 11.205

Review 4.  Homotropic allosteric regulation in monomeric mammalian glucokinase.

Authors:  Mioara Larion; Brian G Miller
Journal:  Arch Biochem Biophys       Date:  2011-11-15       Impact factor: 4.013

5.  Small-Molecule Allosteric Activation of Human Glucokinase in the Absence of Glucose.

Authors:  Joseph M Bowler; Katherine L Hervert; Mark L Kearley; Brian G Miller
Journal:  ACS Med Chem Lett       Date:  2013-09-05       Impact factor: 4.345

6.  Order-disorder transitions govern kinetic cooperativity and allostery of monomeric human glucokinase.

Authors:  Mioara Larion; Roberto Kopke Salinas; Lei Bruschweiler-Li; Brian G Miller; Rafael Brüschweiler
Journal:  PLoS Biol       Date:  2012-12-18       Impact factor: 8.029

  6 in total

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