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

James S. Scott, Alan M. Birch, Katy J. Brocklehurst, Hayley S. Brown, Kristin Goldberg, Sam D. Groombridge, Julian A. Hudson, Andrew G. Leach, Philip A. MacFaul, Darren McKerrecher, Ruth Poultney, Paul Schofield, Per H. Svensson

Research output: Contribution to journalArticlepeer-review

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.
Original languageEnglish
Pages (from-to)95-100
JournalMedChemComm
Volume4
Issue number1
DOIs
Publication statusPublished - Jan 2013

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