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Issue 1, 2013
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Optimisation of aqueous solubility in a series of G protein coupled receptor 119 (GPR119) agonists

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Abstract

Improving aqueous solubility is a challenge frequently faced within drug discovery programs. Herein we describe increases in solubility in two sub-series of GPR119 agonists through reduction of lipophilicity together with hydrogen bond acceptor modulation. Small molecule X-ray crystallography was utilised to investigate effects on solid state interactions.

Graphical abstract: Optimisation of aqueous solubility in a series of G protein coupled receptor 119 (GPR119) agonists

  • This article is part of the themed collection: New Talent
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Publication details

The article was received on 21 May 2012, accepted on 20 Jun 2012 and first published on 21 Jun 2012


Article type: Concise Article
DOI: 10.1039/C2MD20130E
Citation: Med. Chem. Commun., 2013,4, 95-100
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    Optimisation of aqueous solubility in a series of G protein coupled receptor 119 (GPR119) agonists

    J. S. Scott, A. M. Birch, K. J. Brocklehurst, H. S. Brown, K. Goldberg, S. D. Groombridge, J. A. Hudson, A. G. Leach, P. A. MacFaul, D. McKerrecher, R. Poultney, P. Schofield and P. H. Svensson, Med. Chem. Commun., 2013, 4, 95
    DOI: 10.1039/C2MD20130E

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