title: Microwave-assisted preparation and antimicrobial activity ofO-alkylamino benzofurancarboxylates.
abstract: 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)ethoxy]-6-methoxy-2-benzofurancarboxylate hydrochloride was identified as the most active compound (MIC 3-12 × 10-3μmol/cm3against Gram-positive bacteria; MIC 9.4 × 10-2μmol/cm3againstCandidaandAspergillus brasiliensis). The molecular and crystal structures of 2-(N,N-diethylamino)ethyl 6-acetyl-5-hydroxy-2-methyl-3-benzofurancarboxylate were established by single-crystal X-ray diffraction.
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authors.affiliation: Department of Organic Chemistry, Faculty of Pharmacy, Medical University of Warsaw, 1 Banacha, 02097 Warsaw, Poland.
authors.forename: Kinga
authors.initials: K
authors.lastname: Ostrowska
authors.affiliation: Department of Organic Chemistry, Faculty of Pharmacy, Medical University of Warsaw, 1 Banacha, 02097 Warsaw, Poland.
authors.forename: Elżbieta
authors.initials: E
authors.lastname: Hejchman
authors.affiliation: Department of Crystallography, Faculty of Chemistry, Adam Mickiewicz University, Grunwaldzka 6, 60780 Poznan, Poland.
authors.forename: Irena
authors.initials: I
authors.lastname: Wolska
authors.affiliation: Department of Antibiotics and Microbiology, National Medicines Institute, 30/34 Chełmska, 00725 Warsaw, Poland.
authors.forename: Hanna
authors.initials: H
authors.lastname: Kruszewska
authors.affiliation: Department of Organic Chemistry, Faculty of Pharmacy, Medical University of Warsaw, 1 Banacha, 02097 Warsaw, Poland.
authors.forename: Dorota
authors.initials: D
authors.lastname: Maciejewska
keywords: Alkylation; Drug research; Heterocycles; Phase-transfer catalysis; X-ray structure determination