synthesis and preliminary evaluation of the antimicrobial activity of selected 3-benzofurancarboxylic acid derivatives合成及抗菌活性的初步评价选择3-benzofurancarboxylic酸衍生品.pdf

Molecules 2010, 15, 4737-4749; doi:10.3390/molecule OPEN ACCESS molecules ISSN 1420-3049 /journal/molecules Article Synthesis and Preliminary Evaluation of the Antimicrobial Activity of Selected 3-Benzofurancarboxylic Acid Derivatives Jerzy Kossakowski 1, Mariola Krawiecka 1,*, Bożena Kuran 1, Joanna Stefańska 2 and 3 Irena Wolska 1 Department of Medical Chemistry, Medical University of Warsaw, 3 Oczki Str., 02-007 Warsaw, Poland; E-Mails: jerzy.kossakowski@.pl (J.K.); bozena.kuran@.pl (B.K.) 2 Department of Pharmaceutical Microbiology, Medical University of Warsaw, 3 Oczki Str., 02-007 Warsaw, Poland; E-Mail: joanna.stefanska@.pl (J.S.) 3 Department of Crystallography, Faculty of Chemistry, Adam Mickiewicz University, 6 Grunwaldzka Str., 60-780 Poznań, Poland; E-Mail: iwolska@.pl (I.W.) * Author to whom correspondence should be addressed; E-Mail: mariola.krawiecka@.pl. Received: 1 June 2010; in revised form: 29 June 2010 / Accepted: 1 July 2010 / Published: 6 July 2010 Abstract: Halogen derivatives of selected 3-benzofurancarboxylic acids were prepared using 6-acetyl-5-hydroxy-2-methyl-3-benzofuranocarboxylic acid as starting material. 1H- NMR spectra were obtained for all of the synthesized structures, and for compound VI, an X-ray crystal structure was also obtained. All derivatives were tested for antimicrobial activity against a selection of Gram-positive cocci, Gram-negative rods and yeasts. Three compounds, III, IV, and VI, showed antimicrobial activity against Gram-positive