Microwave-assisted preparation and antimicrobial activity of O-alkylamino benzofurancarboxylates

摘要

A series of derivatives of 2 and 3-benzofurancarboxylates were synthesized under microwave-assisted conditions. Their in-vitro antimicrobial properties were assessed. Inhibition by the compounds of the growth of antibiotic-susceptible standards and clinically isolated strains of Gram-positive and Gram-negative bacteria, yeasts, and a human fungal pathogen was moderate to significant. Methyl 5-bromo-7-[2-(N,N-diethylamino)efh-oxy]-6-methoxy-2-benzofurancarboxylate hydrochloride was identified as the most active compound (MIC 3-12 x 10~(-3) μmol/cm~3 against Gram-positive bacteria; MIC 9.4 x 10~(-2) μmol/cm~3 against Candida and Aspergillus brasiliensis). The molecular and crystal structures of 2-(N,N-diethylairuno)ethyl 6-acetyl-5-hydroxy-2-methyl-3-benzofurancarboxylate were established by single-crystal X-ray diffraction.