Polymethoxyflavones (PMFs) from citrus peels possess multiple biological activities such as antioxidant, inhibitory effects against chronic inflammation and chemoprevention. However, both aqueous and lipid solubility of PMFs is poor, which hiders the evaluation of the biological activity of PMFs. In this study, a version of lipophilic prodrugs of 5-demethylnobiletin was synthesized for the bioactivity testing. Nobiletin was first demethylated in aqueous ethanol with the catalysis of hydrochloric acid. The resulted 5-demethylnobiletin was esterified with lauric acid under a coupling reagent or lauroyl chloride in the presence of an amine base such as triethylamine. Detailed reaction conditions will be reported.

Synthesis and biological activity evaluation of 5-demethylnobiletin prodrugs

ACS Spring Meeting 2021

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.