Synthèse et évaluation biologique de prodrogues de phosphonates à visée thérapeutique, le foscarnet et le PALA

MONTPELLIER-BU Sciences (341722106) / SudocSudocFranceF

Influence of the benzyloxycarbonyl protective group on glycosylation with mannopyranosil donors

International audienc

Synthesis and receptor binding affinity of carboxylate analogues of the mannose 6-phosphate recognition marker.

The mannose 6-phosphate/insulin-like growth factor II receptor (M6P/IGF2R) is involved in multiple physiological pathways including targeting of lysosomal enzymes, degradation of IGF2, and cicatrization through TGFbeta activation. To target potential therapeutics to this membrane receptor, four carboxylate analogues of mannose 6-phosphate (M6P) were synthesized. Three of them, two isosteric carboxylate analogues and a malonate derivative, showed a binding affinity for the M6P/IGF2R equivalent to or higher than that of M6P. Contrary to M6P, all these analogues were particularly stable in human serum. Moreover, these derivatives did not present any cytotoxic activity against two human cell lines. These analogues represent a new potential for the lysosomal targeting of enzyme replacement therapy in lysosomal diseases or to prevent the membrane-associated activities of the M6P/IGF2R

Encapsulation and release of a fluorescent probe, khusimyl dansylate, obtained from vetiver oil by complex coacervation.

International audienc

Homologation of carboxylic acids by arndt-eistert reaction under ultrasonic waves

International audienc

A convenient synthesis of peracetylated glycosyl halides using bismuth(III) halides as catalysts

International audienc

Valorization Of Brazilian Vetiver (vetiveria Zizanioides (l.) Nash Ex Small) Oil.

The valorization of extracts from Brazilian vetiver (Vetiveria zizanioides (L.) Nash ex Small) roots was studied. This study took into account the extraction method, the chemical composition of the extracts, their sensorial characteristics, and the possibility of chemical transformations of the product. The performed extraction methods were hydrodistillation and extraction with supercritical carbon dioxide. Some pretreatment methods were tested on the vetiver roots and evaluated in terms of extraction yield, process time, chemical composition, and sensorial properties. Supercritical carbon dioxide extraction resulted in high yield (3.2%) in significantly less time than the other methods. The chemical compositions of the extracts obtained by the different methods were also compared to those of commercial vetiver oils from other sources, showing that Brazilian samples had a greater acid amount. An extraction in basic medium from Brazilian vetiver oil was done to remove its main acid (zizanoic acid), which was chemically transformed into an alcohol (khusimol) of desirable sensorial properties. Sensory evaluation indicated that the Brazilian volatile oil without acid could be used in perfumery and the extract obtained with supercritical carbon dioxide could have application in food.526578-8