In 2019, the Laphookhieo group isolated a series of molecules from the twig extract of Dasymaschalon dasymaschalum. Two of these are structural variants of paprazine and were found to inhibit a-glucosidase, a key enzyme in sugar metabolism, with greater potency than the diabetes drugs acarbose and miglitol. Thus, these molecules may serve as templates for future diabetes drugs. In this presentation, I will summarize our work toward synthesizing the target paprazine derivatives in question, as well as 10 additional analogs, all for the ultimate purpose of carrying out a structure-activity-relationship (SAR) study of this family, in order to better understand which features contribute to its a-glucosidase inhibition activity.

Synthesis and testing of paprazine derivatives

ACS Spring 2022

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