a study of fluorinated β-nitrostyrenes as antimicrobial agents氟化β-nitrostyrenes作为抗菌药物的研究.pdfVIP

Appl. Sci. 2012, 2, 114-128; doi:10.3390/app2010114 OPEN ACCESS applied sciences ISSN 2076-3417 /journal/applsci Article A Study of Fluorinated β-Nitrostyrenes as Antimicrobial Agents King Lo, Hugh Cornell, Gina Nicoletti, Neale Jackson and Helmut Hügel * Health Innovations Research Institute School of Applied Sciences, RMIT University, Melbourne, 3001 Australia; E-Mails: s3185155@.au (K.L.); hugh.cornell@.au (H.C.); gina.nicoletti@.au (G.N.); neale.jackson@.au (N.J.) * Author to whom correspondence should be addressed; E-Mail: helmut.hugel@.au; Tel.: +61-3-9925-2626; Fax: +61-3-9925-3747. Received: 23 January 2012; in revised form: 10 February 2012 / Accepted: 14 February 2012 / Published: 23 February 2012 Abstract: The effect of variously fluorine-substituted β-methyl-β-nitrostyrenes on their antimicrobial activity was investigated. Their efficacy was determined by minimum inhibition concentration (MIC) in cultures of Gram positive and Gram negative bacteria and a fungus. Highest activity against the Gram negative bacterium, E.coli, was achieved with 4-fluorine-aryl substituted β-methyl-β-nitrostyrenes, while most compounds gave excellent results against gram positive bacteria. Importantly, the addition of the β-methyl group profoundly enhanced the antibacterial activity of the compounds tested. The comparative KD values for the most potent compounds against E.coli were much lower than tho