160801-26-3Relevant articles and documents
Unsaturated acyl chains dramatically enhanced cellular uptake by direct translocation of a minimalist oligo-arginine lipopeptide
Swiecicki,Di Pisa,Lippi,Chwetzoff,Mansuy,Trugnan,Chassaing,Lavielle,Burlina
, p. 14656 - 14659 (2015)
The recurring issue with cell penetrating peptides is how to increase direct translocation vs. endocytosis, to avoid premature degradation. Acylation by a cis unsaturated chain (C22:6) of a short cationic peptide provides a new rational design to favour diffuse cytosolic and dense Golgi localisations.
STRUCTURED MOLECULAR VECTORS FOR ANTI-INFLAMMATORY COMPOUNDS AND USES THEREOF
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Page/Page column 44, (2020/09/08)
The present invention relates to structured molecular vectors of formula (I), compounds of formula (II) and pharmaceutical compositions comprising such compounds. The invention also relates to such pharmaceutical compositions for use for preventing and/or treating a disease chosen among an inflammatory disease or a disease associated with a cognitive disorder. The invention further relates to such pharmaceutical compositions for use for preventing cognitive decline or restoring cognitive functions altered in brain injuries and/or in traumatic brain injuries and/or in a neuroinflammatory disease, and/or in a neurodegenerative disease.
Method of synthesizing acetonide-protected catechol-containing compounds and intermediates produced therein
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Page/Page column 27-28, (2012/07/30)
The inventors disclose here a novel, facile approach to the synthesis of acetonide-protected catechol-containing compounds having at least one amine group. In specific embodiments, the invention provides novel methods of synthesizing 3,4-dihydroxyphenylalanine (H-DOPA(acetonide)-OH (6)), Fmoc-protected H-DOPA(acetonide)-OH (Fmoc-DOPA(acetonide)-OH (7)), Fmoc-protected dopamine (Fmoc-dopamine(acetonide) (10)), TFA-protected dopamine (TFA-dopamine(acetonide) (13)) and acetonide-protected 4-(2-aminoethyl)benzene-1,2-diol (acetonide-protected dopamine (14)).