Background: Oleanolic Acid (OA) is a ubiquitous product of triterpenoid compounds.
Due to its inexpensive availability, unique bioactivities, pharmacological effects and non-toxic
properties, OA has attracted tremendous interest in the field of drug design and synthesis. Furthermore,
many OA derivatives have been developed for ameliorating the poor water solubility and bioavailability.
Objective: Over the past few decades, various modifications of the OA framework structure have led
to the observation of enhancement in bioactivity. Herein, we focused on the synthesis and medicinal
performance of OA derivatives modified on A-ring. Moreover, we clarified the relationship between
structures and activities of OA derivatives with different functional groups in A-ring. The future application
of OA in the field of drug design and development also was discussed and inferred.
Conclusion: This review concluded the novel achievements that could add paramount information
to the further study of OA-based drugs.