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

• 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.

Subject headings

NATURVETENSKAP  -- Biologi -- Biokemi och molekylärbiologi (hsv//swe)

NATURAL SCIENCES  -- Biological Sciences -- Biochemistry and Molecular Biology (hsv//eng)

Keyword

Stimulated Insulin-Secretion

Medicinal Chemistry

Glycemic Control

Discovery

Potent

G-Protein-Coupled-Receptor-119

As1535907

Release

Agent

Publication and Content Type

ref (subject category)

art (subject category)