Jump to main content
Jump to site search

Issue 9, 2012
Previous Article Next Article

Property based optimisation of glucokinase activators – discovery of the phase IIb clinical candidate AZD1656

Author affiliations

Abstract

Glucokinase plays a central role in glucose homeostasis and small molecule activators of the glucokinase enzyme have been the subject of significant pharmaceutical research in the quest for agents capable of delivering improved glycaemic control. Here we describe our medicinal chemistry campaign to improve on our previously described development candidate in this area, AZD1092, focussed on removal of Ames liability and improved permeability characteristics. This work culminated in the superior compound AZD1656 which has progressed to phase 2 clinical trials.

Graphical abstract: Property based optimisation of glucokinase activators – discovery of the phase IIb clinical candidate AZD1656

Back to tab navigation

Supplementary files

Publication details

The article was received on 22 Mar 2012, accepted on 13 Jun 2012 and first published on 18 Jun 2012


Article type: Concise Article
DOI: 10.1039/C2MD20077E
Med. Chem. Commun., 2012,3, 1077-1081

  •   Request permissions

    Property based optimisation of glucokinase activators – discovery of the phase IIb clinical candidate AZD1656

    M. J. Waring, D. S. Clarke, M. D. Fenwick, L. Godfrey, S. D. Groombridge, C. Johnstone, D. McKerrecher, K. G. Pike, J. W. Rayner, G. R. Robb and I. Wilson, Med. Chem. Commun., 2012, 3, 1077
    DOI: 10.1039/C2MD20077E

Search articles by author

Spotlight

Advertisements