Brigitte Lesur

New deoxynojirimycin derivatives as potent inhibitors of intestinal α-glucohydrolases

Abstract New N-alkyl, alkenyl and benzyl substituted DNJ derivatives incorporating a silicon atom in the substituent were synthesised. Kinetic parameters ( K i , t 1 2 ) for inhibition of rat intestinal α-glucohydrolases as well as human lysosomal α-glucosidases were measured. New DNJ derivatives are potent and selective inhibitors of intestinal α-glucohydrolases.

Design and synthesis of a series of indole glycoprotein IIb/IIIa inhibitors.

Synthesis of 1,3-disubstituted indoles derivatives as potential glycoprotein (GP) IIb/IIIa antagonists was reported. Substitution of the indolic nitrogen atom by piperidino or benzamidino moieties was used as mimics of an arginine residue. The acid carboxylic group was linked to the indole scaffold in position-3 via a methylene unit (compounds 4, 9, 10). Introduction of a beta-alanine chain was carried out on the acids (17-22) which after deprotection and basic hydrolysis afforded the final compounds 39-46. The distance between the indole scaffold and the amide bond was modulated from no methylene unit (compound 39) to 1 (compounds 40, 41) or 2 methylene units (compounds 42-46). The presence of a tosylamino group on the beta-alanine chain (compound 56) slightly increased the inhibiting action on platelet aggregation initiated by collagen.

Aryl-Heteroaryl Derivatives as Novel Wake-Promoting Agents

In search of a next generation molecule to the novel wake‐promoting agent modafinil, a series of aryl‐heteroayl‐derived wakefulness enhancing agents (in rats) was developed. From this work, compound 16 was separated into its enantiomers to profile them individually.

Wake-promoting agents: search for next generation modafinil: part IV.

In search of a next generation molecule to the novel wake promoting agent modafinil, a series of diphenyl ether derived wakefulness enhancing agents (in rat) was developed. From this work, racemic compound 16 was separated into its chiral enantiomers to profile them individually.