AUTHOR=Long Junjun , Ji Wentao , Zhang Doudou , Zhu Yifei , Bi Yi 

TITLE=Bioactivities and Structure–Activity Relationships of Fusidic Acid Derivatives: A Review

JOURNAL=Frontiers in Pharmacology

VOLUME=12

YEAR=2021

URL=https://www.frontiersin.org/journals/pharmacology/articles/10.3389/fphar.2021.759220

DOI=10.3389/fphar.2021.759220

ISSN=1663-9812

ABSTRACT=<p>Fusidic acid (FA) is a natural tetracyclic triterpene isolated from fungi, which is clinically used for systemic and local <italic>staphylococcal</italic> infections, including methicillin-resistant <italic>Staphylococcus aureus</italic> and coagulase-negative <italic>staphylococci</italic> infections. FA and its derivatives have been shown to possess a wide range of pharmacological activities, including antibacterial, antimalarial, antituberculosis, anticancer, tumor multidrug resistance reversal, anti-inflammation, antifungal, and antiviral activity <italic>in vivo</italic> and <italic>in vitro</italic>. The semisynthesis, structural modification and biological activities of FA derivatives have been extensively studied in recent years. This review summarized the biological activities and structure–activity relationship (SAR) of FA in the last two decades. This summary can prove useful information for drug exploration of FA derivatives.</p>