MFELE NTSA Jeanine, KILEMBE THAMBWE Jason, NTUMBA KANKOLONGO Joséphine, TABA KALULU Muzele, TSHIONGO MUAMBA T. Christian*

Synthesis, Antibacterial Activity Evaluation and Structure-Activity Relationship Study of Some Ibuprofene Analogues
In order to highlight the various electronic, steric and lipophilic contributions responsible for the antibacterial activity of Ibuprofen, we studied the structure-activity relationship of some synthetic analogues of Ibuprofen. Those analogues were synthesized and characterized. The antibacterial activity was evaluated by microdilution method using Staphylococcus aureus and Pseudomonas fluorescens as strains. Evaluation of the influence of structural modifications on biological activity (antibacterial activity) shows that electronic contributions (calculated by the software Chemdraw and Gaussian) were the major property influencing the antibacterial activity. The ethyl ester derivate highlighted the lipophilic contribution. The nitro derivate obtained with 69% yield showed the best antibacterial activity. This analog can be a starting point for the development of a generation of antibacterial based on Ibuprofen structure. Télécharger l'article