17S,20S-Methanofusidic acid,a new potent semi-synthetic fusidane antibiotic |
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Authors: | Duvold Tore Jørgensen Anne Andersen Niels R Henriksen Anne S Dahl Sørensen Morten Björkling Fredrik |
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Affiliation: | LEO Pharma, Industriparken 55, DK-2750, Ballerup, Denmark |
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Abstract: | A novel fusidic acid type antibiotic having the side chain linked to the tetracyclic ring system via a spiro-cyclopropane system is described. 17S,20S-Methanofusidic acid is obtained by an efficient synthetic route including cyclopropanation of the Δ17(20) bond with attack solely from the least hindered -face. The spiro-cyclopropane system orients the side chain into a bioactive conformational space. The new 17S,20S-methanofusidic acid exerts antibacterial activity against several Gram-positive species with potency essentially equal to natural fusidic acid. |
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