Efficient synthesis and preliminary biological evaluations of trifluoromethylated imidazo[1,2- a ]pyrimidines and benzimidazo[1,2- a ]pyrimidines - Physico-chimie des Matériaux et des Electrolytes pour l'Energie Laboratoire - - EA 6299 Accéder directement au contenu
Article Dans Une Revue New Journal of Chemistry Année : 2019

Efficient synthesis and preliminary biological evaluations of trifluoromethylated imidazo[1,2- a ]pyrimidines and benzimidazo[1,2- a ]pyrimidines

Résumé

Fluoromethylated imidazo[1,2-a]pyrimidines and benzimidazo[1,2-a]pyrimidines were synthesized through Michael addition/intramolecular cyclization reaction by condensation of 2-amino imidazole derivatives with ethyl 4,4,4-trifluorobut-2-ynoate and using C–O bond activation. The synthons thus obtained can be functionalized by forming new chemical bonds, including C–C, C–N and C–S, to provide easy access to a wide range of novel trifluoromethylated imidazo[1,2-a]pyrimidines and benzimidazo[1,2-a]pyrimidines in good to excellent yields. Preliminary biological evaluation revealed a number of derivatives displaying micromolar IC50 values against monoamine oxidase B and butyrylcholinesterase, two important targets in the field of neurodegenerative disorders.
Fichier non déposé

Dates et versions

hal-02268002 , version 1 (20-08-2019)

Identifiants

Citer

Badr Jismy, Mohamed Akssira, Damijan Knez, Gérald Guillaumet, Stanislav Gobec, et al.. Efficient synthesis and preliminary biological evaluations of trifluoromethylated imidazo[1,2- a ]pyrimidines and benzimidazo[1,2- a ]pyrimidines. New Journal of Chemistry, 2019, 43 (25), pp.9961-9968. ⟨10.1039/c9nj01982k⟩. ⟨hal-02268002⟩
55 Consultations
0 Téléchargements

Altmetric

Partager

Gmail Facebook X LinkedIn More