T-0632, a non-peptidic molecule, is a reverse agonist of the GLP-1 receptor, which is involved in the production and release of insulin by the pancreas.  Because of the assumed affinity of T-0632 for the binding site of GLP-1 on GLP-1R, we can use T-0632 to better understand the structure and interactions at this binding site. The preparation of T-0632 analogs can provide a structure-activity relationship for this binding.  T-0632 can be selectively mono-iodinated using mild conditions, and the possibility of a second electrophilic aromatic substitution is implied by preliminary experiments.  The conversion of these halogenated T-0632 analogs into other analogs will be discussed, as will their biological activity.

Synthesis of halogenated analogs of T-0632 to investigate the GLP-1R binding site

245th National Meeting (2013)

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