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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

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Article information


Submitted
21 May 2012
Accepted
20 Jun 2012
First published
21 Jun 2012

Med. Chem. Commun., 2013,4, 95-100
Article type
Concise Article

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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