1.
Bioorg Med Chem
; 21(23): 7453-64, 2013 Dec 01.
Article
in English
| MEDLINE
| ID: mdl-24126093
ABSTRACT
Molecular modeling techniques were applied to the design, synthesis and optimization of a new series of xanthine based adenosine A(2A) receptor antagonists. The optimized lead compound was converted to a PEG derivative and a functional in vitro bioassay used to confirm efficacy. Additionally, the PEGylated version showed enhanced aqueous solubility and was inert to photoisomerization, a known limitation of existing antagonists of this class.