T-0632, a non-peptide, small molecule, acts as an inverse agonist of glucagon-like-peptide-1 receptor (GLP-1R).  The study of T-0632 and its analogs can further the understanding of the structure of GLP-1R. The carboxylic acid side chain of T-0632 is essential to the biological activity, as shown by the failure of a non-carboxylated analog to inhibit binding the natural agonist, GLP-1. The work presented here explores additional modifications of this side chain, with the goal of further refining our understanding of the role of the carboxylic acid in the inhibition of GLP-1R.  Modifications will include changing the polarity, charge, and hydrogen bonding capability of the side chain. Preparation of the analogs will be described, as will preliminary biological results.

Preparation of analogs of the GLP-1R inverse agonist, T-0632

247th National Meeting (2014)

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