Abstract

Some of the naturally occurring fusidic acid-related antibiotics include helvolic acid, cephalosporin P family, and the fusidic acid-related antibiotics formed by Fusidium coccineum. Helvolic acid contains the same skeleton as fusidic acid, but the substitution pattern of rings A, B, and C is different. Its antibacterial properties are qualitatively similar to those of fusidic acid. Fusidic acid inhibits in vivo and in vitro protein synthesis in both prokaryotic and eukaryotic cells. In Staphylococcus aureus, two types of resistance to fusidic acid may occur. One of these involves chromosomal mutations giving rise to modification of the protein-synthesizing machinery. The other type of fusidic acid resistance known to occur in staphylococci is plasmid mediated. This type of resistance results from exclusion of the antibiotic from the bacterial cell. It has been observed that the structure–activity relationships among 16-deacetoxy-16β-alkylthiofusidic acids are very similar to those observed in the 16β-alkoxy series.

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