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.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4346301 | PMC |
| http://dx.doi.org/10.1016/j.bmc.2013.09.043 | DOI Listing |
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