期刊
MONATSHEFTE FUR CHEMIE
卷 144, 期 11, 页码 1679-1689出版社
SPRINGER WIEN
DOI: 10.1007/s00706-013-1067-7
关键词
Heterocycles; Alkylation; Phase-transfer catalysis; X-ray structure determination; Drug research
资金
- Medical University of Warsaw, Faculty of Pharmacy [FW 24/PM1/11]
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 x 10(-3) mu mol/cm(3) against Gram-positive bacteria; MIC 9.4 x 10(-2) mu mol/cm(3) against Candida and Aspergillus 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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