G protein-coupled receptor 55, also known as GPR55, was previously considered a cannabinoid receptor. GPR55 is expressed widely throughout the body, especially in the brain and small intestines along with cells that regulate bone cell function. GPR55's specific physiological role is still unclear; however, it has been linked to involvement in several processes including neuropathic/ inflammatory pain, cancer, and bone physiology. With implicated roles in such important areas of medical interest, it is desirous to synthesize effective antagonists in order to properly characterize the physiological role(s) of GPR55. Computational modeling of GPR55 was utilized to identify lead antagonist molecules. A method of assembly was devised retrosynthetically as shown in   , and the synthesis of a number of analogs is currently under way to better map out GPR55's function and purpose. The results of these synthetic efforts will be herein presented.

Synthesis of polyheterocyclic antagonists of GPR55

248th National Meeting (2014)

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