Issue 1, 2013

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

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

Supplementary files

Article information

Article type
Concise Article
Submitted
21 May 2012
Accepted
20 Jun 2012
First published
21 Jun 2012

Med. Chem. Commun., 2013,4, 95-100

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

To request permission to reproduce material from this article, please go to the Copyright Clearance Center request page.

If you are an author contributing to an RSC publication, you do not need to request permission provided correct acknowledgement is given.

If you are the author of this article, you do not need to request permission to reproduce figures and diagrams provided correct acknowledgement is given. If you want to reproduce the whole article in a third-party publication (excluding your thesis/dissertation for which permission is not required) please go to the Copyright Clearance Center request page.

Read more about how to correctly acknowledge RSC content.

Spotlight

Advertisements