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Dihydroceramide desaturase inhibitors.

Authors: Fabriàs, Gemma; Llebaria, Amadeu; Triola Guillem, Gemma;

Dihydroceramide desaturase inhibitors.

Abstract

[EN]The invention relates to derivatives of cyclopropenylceramide used as desaturase inhibitors characterised by the general formula I, wherein R1 may be an alkyl, alkenyl, alkynyl, aryl or any heterocyclic group, n can have any value whatsoever, be branched or not and contain unsaturations, and R2 and R3 can have the same or different values, represent aryl, heteroaryl, alkyl or acyl groups with one or more unsaturations in the chain, which may be branched or not and substituted by OH groups. The members of this new class of compounds have demonstrated an extraordinary activity as inhibitors of dihydroceramide desaturase and of ceramide biosynthesis and are useful for the treatment of pathologies associated with increases in intracellular ceramide levels. [ES]Derivados de ciclopropenilceramida como inhibidores de desaturasas caracterizados por la fórmula general I, en la que R1 puede ser un grupo alquilo, alquenilo, alquinilo, arilo o cualquier heterociclo, n puede tener cualquier valor y estar ramificada o no y contener insaturaciones y R2 y R3 pueden tener el mismo o distinto valor, representan grupos arilo, heteroarilo, alquilo o acilo con una o varias insaturaciones en la cadena, que puede estar ramificada o no, y sustituida con grupos OH. Miembros de esta nueva clase de compuestos han mostrado una extraordinaria actividad como inhibidores de la dihidroceramida desaturasa y de la biosíntesis de ceramida y son de utilidad para el tratamiento de patologias asociadas a aumentos en los niveles de ceramida intracelular.

Fecha de solicitud:14.12.2002.- Titular: Consejo Superior de Investigaciones Científicas (CSIC).

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selected citations
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This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
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popularity
This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.
BIP!Popularity provided by BIP!
influence
This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
BIP!Influence provided by BIP!
impulse
This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.
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