Synthesis of arylfuran derivatives as potential antimicrobial agents

Drugs used as antimicrobials have several limitations regarding the safety and efficacy.1,2 As examples we can mention the quinolone and fluoroquinolone antibiotics whose consumption and rate of resistance has been increasing around the world.3 In this context, seven furan derivatives were evaluated for their antimicrobial potential against a panel of Gram-negative and Gram-positive bacteria. Compounds 2 and 4 (Figure) displayed antibacterial activity (MIC = 100-500 µM) for both gram-negative (P. aeruginosa) and gram-positive (S. aureus and S. agalactiae) bacteria, suggesting that these compounds may exhibit a broad spectrum of action. In silico studies were performed to investigate the drug-like properties and toxicity profile of the active compounds. Based on these studies, arylfurans 2 and 4 exhibit physicochemical properties appropriate for oral administration and were predicted to be well tolerated (minimum toxic dose >50 mg.kg-1). These results indicate that 2 and 4 are promising compounds for further studies.