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Issue 8, 2011
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Matrix-based multiparameter optimisation of glucokinase activators: the discovery of AZD1092

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Abstract

Small molecule activators of the glucokinase enzyme have the potential to deliver a level of glycaemic control that is superior to current oral agents and hence have great promise as new therapies for Type 2 Diabetes. As such, attempts to discover glucokinase activators suitable for clinical development have been the focus of many major pharmaceutical research programmes. Here we show how property-based matrix optimisation has been used to improve the multi-parameter technical profile of the AstraZeneca series of glucokinase activators culminating in the discovery of the development candidate AZD1092.

Graphical abstract: Matrix-based multiparameter optimisation of glucokinase activators: the discovery of AZD1092

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Publication details

The article was received on 30 Mar 2011, accepted on 31 May 2011 and first published on 28 Jun 2011


Article type: Concise Article
DOI: 10.1039/C1MD00092F
Med. Chem. Commun., 2011,2, 775-779

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    Matrix-based multiparameter optimisation of glucokinase activators: the discovery of AZD1092

    M. J. Waring, C. Johnstone, D. McKerrecher, K. G. Pike and G. Robb, Med. Chem. Commun., 2011, 2, 775
    DOI: 10.1039/C1MD00092F

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