Abstract
Fusidic acid (FA) is a natural tetracyclic triterpene isolated from fungi, which is clinically used for systemic and local staphylococcal infections, including methicillin-resistant Staphylococcus aureus and coagulase-negative staphylococci 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 in vivo and in vitro. 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.
Highlights
Over the past 40 years, more than half of the new chemical entities approved for the treatment of various diseases have originated from unmodified natural products, their semi-synthetic derivatives, or synthetic biological analogs (Newman and Cragg, 2020)
Shakurova et al synthesized three quaternary pyridinium salts and tetrahydropyridine derivatives (7, 8, and 9) of Fusidic acid (FA) using an effective one-pot method, but after antimicrobial screening, the results showed that there was no inhibitory activity against the tested strains when the concentration of the derivatives was 32 μg/ml (Shakurova et al, 2019)
FA can be obtained by fermentation, and has attracted increasing attention in recent years
Summary
Over the past 40 years, more than half of the new chemical entities approved for the treatment of various diseases have originated from unmodified natural products, their semi-synthetic derivatives, or synthetic biological analogs (Newman and Cragg, 2020). Natural products are rich in structural types and have a wide range of biological activities, and are the main source for the discovery of new chemical entities and lead compounds (Chen et al, 2017; Agarwal et al, 2020). FA and its derivatives have been shown to possess a wide range of pharmacological activities, including antibacterial The SARs of FA and its derivatives in antibacterial, antiparasitic, antituberculosis, antitumor and tumor MDR reversal were summarized. This review provides useful information for the development of FA derivatives and gives a direction for further inspiration to enrich its structures with good pharmacological activities
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