Abstract

ANTIBACTERIAL ACTIVITY OF IMIDAZO [1,2-α] PYRIDINYLCHALCONES DERIVATIVES AGAINST ENTEROCOCCUS FAECALIS

Déto U. Jean – Paul N'guessan, Mahama Ouattara*, Songuigama Coulibaly, Mamidou W. Kone, Drissa Sissouma

Abstract

The emergence of nosocomial strains of Enterococcus faecalis and drug resistance that antibiotics faces in the treatment of enterococcal infections, prompted us searching for new more efficient bioactive molecules For this purpose, 10 chalcones based imidazo[1,2-a]pyridine (5a-5d) were synthesized and assessed for their antibacterial activity against susceptible and resistant strains of Enterococcus faecalis. The screening was fulfilled using the agar diffusion method to select best molecule, then by the method of dilution in liquid medium compared to Amoxicillin and Gentamicin. The compounds 5h and 5d, with respective MIC 44.6 μM and 9.9 μM, exhibited the best antibacterial profiles. It appears from the structure activity relationship studies that the presence of fluorine on the benzene homocycle or replacement of this homocycle by a furan ring lead to significant antibacterial activities. Paradoxically, all activities were more effective against resistant strains than on sensitive ones. Compounds 5h and 5d may constitute seeds of a new class of antibacterial effective against resistant Enterococcus faecalis.

Keywords: imidazo[1,2-a]pyridine, Chalcone, Antibacterial activity, Enterococcus faecalis.