Polyene antibiotics, compositions containing said...

Details Polyene antibiotics, compositions containing said... Polyene antibiotics, compositions containing said...

C - Chemistry, Metallurgy

07

H

C07H 17/08 (2006.01) A61P 31/00 (2006.01) C12P 19/62 (2006.01)

Patent

CA 2602355

The invention relates to novel polyenes having formula (I), wherein: R1 represents alkyl, C1-C3; and R2 represents a functional group selected from CH3- or CONH2- (methyl or primary amide). The aforementioned polyenes have a biocide action on organisms comprising cell membranes that contain ergosterol, e.g. fungi or parasites. Said compounds can be obtained using a method that consists in cultivating a producing micro-organism under conditions that enable the production thereof. In addition, the invention also relates to a mechanism for the in vitro production of amidated polyenes, consisting in incubating carboxylated polyenes with cell-free extracts (or proteinaceous fractions) of the producers of same in the presence of ATP/Mg++ and an amide- group donor compound (preferably glutamine).

L'invention concerne des nouveaux polyènes de formule (I) dans laquelle : R1 représente alkyle, C1-C3 ; R2 représente un groupe fonctionnel sélectionné parmi CH3- ou CONH2- (méthyle ou amide primaire). Les polyènes de l'invention présentent une activité biocide contre des organismes qui possèdent des membranes cellulaires contenant de l'ergosterol, par exemple, des champignons ou des parasites. Ces composés peuvent être obtenus au moyen d'un procédé qui consiste à cultiver un micro-organisme producteur dans des conditions qui permettent sa production. L'invention concerne également un mécanisme pour l'obtention in vitro de polyènes amidés qui consiste à incuber des polyènes carboxylés avec des extraits acellulaires (ou des fractions protéiques) de leurs producteurs en présence d'ATP/Mg++ et d'un composé donneur de groupes amides (de préférence de la glutamine).

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