synthesis and antibacterial evaluation of a new series of n-alkyl-2-alkynyl(e)-alkenyl-4-(1h)-quinolones合成和抗菌评估一系列新的n-alkyl-2-alkynyl(e)-alkenyl-4u2014u2014(1 h)喹诺酮类.pdf

Molecules 2012, 17, 8217-8240; doi:10.3390/molecule OPEN ACCESS molecules ISSN 1420-3049 /journal/molecules Article Synthesis and Antibacterial Evaluation of a New Series of N-Alkyl-2-alkynyl/(E)-alkenyl-4-(1H)-quinolones Abraham Wube 1, Juan-David Guzman 2,3, Antje Hüfner 4, Christina Hochfellner 1, Martina Blunder 1, Rudolf Bauer 1, Simon Gibbons 3, Sanjib Bhakta 2 and Franz Bucar 1,* 1 Department of Pharmacognosy, Institute of Pharmaceutical Sciences, Karl-Franzens-University Graz, Universitätsplatz 4, A-8010 Graz, Austria; E-Mails: abraham.wube@uni-graz.at (A.W.); christina.hochfellner@uni-graz.at (C.H.); martina.blunder@uni-graz.at (M.B.); rudolf.bauer@uni-graz.at (R.B.) 2 Department of Biological Sciences, Institute of Structural and Molecular Biology, Birkbeck, University of London, Malet Street, London WC1E 7HX, UK; E-Mails: talauma@ (J.-D.G.); s.bhakta@bbk.ac.uk (S.B.) 3 Department of Pharmaceutical and Biological Chemistry, UCL School of Pharmacy, 29-39 Brunswick Square, London WC1N 1AX, UK; E-Mail: simon.gibbons@ucl.ac.uk 4 Department of Pharmaceutical Chemistry, Institute of Pharmaceutical Sciences, Karl-Franzens-University Graz, Universitätsplatz 1, A-8010 Graz, Austria; E-Mail: antje.huefner@uni-graz.at * Author to whom correspondence should be addressed; E-Mail: franz.bucar@uni-graz.at; Tel.: +43-316-380-5531; Fax: +43-316-380-9860. Received: 10 April 2012; in revised form: 12 June 2012 / Accepted: 15 June 2012 / Published: 9 July 2012 Abstract: To gain further insight into the structural requirements of the aliphatic group at