Aureobasidins

Details Aureobasidins Aureobasidins

C - Chemistry, Metallurgy

07

K

C07K 11/02 (2006.01) A61K 38/15 (2006.01) A61P 31/04 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2157047

This invention relates to Aureobasidins useful as an antifungal agent having broader spectruro. The compound according to this invention includes acyclic depsipeptide consisting of one hydroxy acid residue having A', 3 amino acid residues having C1, F1 and H1, respectively, 4 N- methylamino acid residues having B1; D1, G1and I1, respectively, and 1 cyclic amino acid residue having E1. The typical compound includes one wherein A1 is CH3CH2CH(CH3)-, B1 is (CH3)2CH-, C1 is benzyl, cyclohexylmethyl, p-fluorobenzyl, benzyloxymethyl, benzyloxybenzyl, methoxybenzyl, cyclohexylmethyloxybenzyl or the like, D1 is methyl, benzyl, hydroxymethyl or the like, E1 is -(CH2)3-, F1 is CH3CH2CH(CH3)-, G1 is (CH3)2CH-, H1 is (CH3)2CHCH2- and I1 is (CH3)2C(OH)-. The compound according to this invention has an excellent activity against not only Candida but also Cryptococcus and Aspergillus.

L'invention concerne des auréobasidines utiles en tant qu'agents antimycosiques à large spectre. Ce sont des cyclodepsipeptides se composant d'un reste d'acide hydroxy comprenant le groupe A<1>, de trois restes d'aminoacide comprenant les groupes C<1>, F<1> et H<1>, de quatre restes d'acide N-méthylamino comprenant les groupes B<1>, D<1>, G<1> et I<1>, et d'un reste d'aminoacide cyclique comprenant E<1>. Dans un exemple représentatif de ces composés, A<1> correspond à CH3CH2CH(CH3), B<1> représente (CH3)2CH-, C<1> représente benzyle, cyclohexylméthyle, p-fluorobenzyle, benzyloxyméthyle, méthoxybenzyle, cyclohexylméthyloxybenzyle, etc, D<1> représente méthyle, benzyle, hydroxyméthyle, etc, E<1> représente propylène, F<1> correspond à CH3CH2CH(CH3)-, G<1> à (CH3)2CH-, H<1> à (CH3)2CHCH2-, et I<1> à (CH3)2C(OH). Ces auréobasidines présentent d'excellentes activités non seulement anti-candida mais également anti-cryptococcus et anti-aspergillus.

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