Literature DB >> 15808477

Discovery, synthesis and biological evaluation of novel glucokinase activators.

Darren McKerrecher1, Joanne V Allen, Suzanne S Bowker, Scott Boyd, Peter W R Caulkett, Gordon S Currie, Christopher D Davies, Mark L Fenwick, Harold Gaskin, Emma Grange, Rod B Hargreaves, Barry R Hayter, Roger James, Keith M Johnson, Craig Johnstone, Clifford D Jones, Sarah Lackie, John W Rayner, Rolf P Walker.   

Abstract

The identification, synthesis and SAR of a novel series of glucokinase activators is described. The interplay between lipophilicity, potency and physical properties is discussed, and compound 22 highlighted as having a suitable balance. In vivo pharmacokinetic and acute efficacy studies on this compound are also presented.

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Year:  2005        PMID: 15808477     DOI: 10.1016/j.bmcl.2005.01.087

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


  5 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

2.  Predictive blood glucose lowering efficacy by Glucokinase activators in high fat fed female Zucker rats.

Authors:  G J Coope; A M Atkinson; C Allott; D McKerrecher; C Johnstone; K G Pike; P C Holme; H Vertigan; D Gill; M P Coghlan; B Leighton
Journal:  Br J Pharmacol       Date:  2006-08-21       Impact factor: 8.739

3.  Discovery of a novel site regulating glucokinase activity following characterization of a new mutation causing hyperinsulinemic hypoglycemia in humans.

Authors:  Nicola L Beer; Martijn van de Bunt; Kevin Colclough; Christine Lukacs; Paul Arundel; Constance L Chik; Joseph Grimsby; Sian Ellard; Anna L Gloyn
Journal:  J Biol Chem       Date:  2011-03-29       Impact factor: 5.157

4.  Comparative docking assessment of glucokinase interactions with its allosteric activators.

Authors:  Vandana Kumari; Chenglong Li
Journal:  Curr Chem Genomics       Date:  2008-12-30

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

  5 in total

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