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

Autor:	Katy J. Brocklehurst, Paul Schofield, James S. Scott, Per H. Svensson, Sam D. Groombridge, Kristin Goldberg, Ruth Poultney, Darren Mckerrecher, Julian A. Hudson, Andrew G. Leach, Hayley S. Brown, Philip A. MacFaul, Alan Martin Birch
Rok vydání:	2013
Předmět:	Pharmacology Drug discovery Hydrogen bond Chemistry Organic Chemistry Pharmaceutical Science Biochemistry Combinatorial chemistry Small molecule GPR119 Drug Discovery Aqueous solubility Lipophilicity Molecular Medicine Organic chemistry Solubility G protein-coupled receptor
Zdroj:	MedChemComm. 4:95-100
ISSN:	2040-2511 2040-2503
DOI:	10.1039/c2md20130e
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::e4ada7177556dab7308ef00895d296da https://doi.org/10.1039/c2md20130e Zobrazit plný text záznamu