Xenorxides with antibacterial and antimycotic properties

C - Chemistry – Metallurgy – 12 – P

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C12P 17/18 (2006.01) A61K 31/40 (2006.01) C07D 495/04 (2006.01)

Patent

CA 2217957

The invention is drawn to novel antibiotics, XENORXIDES of formula (A) or (B), wherein R1, R2 = hydrogen, substituted or unsubstituted alkyl, cycloalkyl, acyl, aryl, aralkyl, or heterocyclyl group; R3 = hydrogen, alkyl, cycloalkyl, aralkyl or aryl group, produced by bacterial symbiont Xenorhabdus bovienii and/or other Xenorhabdus species, and/or by oxidation of the corresponding dithiolopyrrolone derivatives with oxygen and Xenorhabdus species, and/or its cell-free filtrate, the additional salts thereof, the compositions thereof and their use as medicaments and/or agrochemicals, particularly in the treatment of infectious diseases involving microorganisms susceptible to them, including drug-resistant Staphylococcus.

L'invention concerne des antibiotiques d'un type nouveau, les XENORXIDES, de formule (A) ou (B), dans laquelle R¿1?, R¿2? représentent hydrogène, un groupe alkyle, cycloalkyle, acyle, aryle, aralkyle ou hétérocyclyle substitué ou non; où R¿3? représente hydrogène, un groupe alkyle, cycloalkyle, aralkyle ou aryle, produits par le symbiote bactérien Xenorhabdus bovienii et/ou d'autres espèces de Xenorhabdus, et/ou par oxydation des dérivés correspondants à base de dithiolopyrrolone par l'oxygène et l'espèce Xenorhabdus, et/ou son filtrat acellulaire, l'invention concerne les sels additionnels de ces antibiotiques, les compositions à base de ces derniers et leur utilisation comme médicaments et/ou comme produits agrochimiques, notamment dans le traitement de maladies infectieuses faisant intervenir des micro-organismes qui y sont sensibles, y compris le Staphylococcus résistant aux médicaments.

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