Synthesis of arylfuran derivatives as potential antibacterial agents

AbstractBacterial infections represent a serious health care problem mainly due to the misuse and overuse of antibiotics, with consequent emergence of multidrug resistant bacterial strains. Then, because the urgent need to find novel and alternative antibacterial agents, the present work focuses on the synthesis of arylfuran derivatives with potential antimicrobial activity. Eighteen arylfuran derivatives were synthesized and evaluated for their antibacterial activity againstStaphylococcus aureus,Escherichia coli andPseudomonas aeruginosa. Among them, seven compounds containing an amino group in their structure showed activity, with compound24 being the most effective against both Gram-negative (E. coli, MIC  = 49 µM) and Gram-positive (S. aureus, MIC  = 98 µM) bacteria, besides having exhibited a modest activity againstP. aeruginosa (MIC  = 770 µM). In addition, based on in silico studies, this is a druglike compound since it does not violate any rules for predicting oral bioavailability. In this context, the significant antibacterial potential and the low similarity with known antibiotics indicate the innovative aspect of co mpound24.
Source: Medicinal Chemistry Research - Category: Chemistry Source Type: research