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Updated: Sep 28, 2026

An Efficient Method for the Synthesis of Peptoids with Mixed Lysine-type/Arginine-type Monomers and Evaluation of Their Anti-leishmanial Activity
Published on: November 2, 2016
17S,20S-Methanofusidic acid, a new potent semi-synthetic fusidane antibiotic
Tore Duvold1, Anne Jørgensen, Niels R Andersen
1LEO Pharma, Industriparken 55, DK-2750 Ballerup, Denmark. tore.duvold@leo-pharma.com
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 Delta17(20) bond with attack solely from the least hindered alpha-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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