Salicylanilide Acetates Synthesis and Antibacterial Evaluation 英文参考文献.docVIP

Molecules 2007, 12, 1-12 molecules ISSN 1420-3049 Full Paper Salicylanilide Acetates: Synthesis and Antibacterial Evaluation Jarmila Vinsova 1,*, Ales Imramovsky 1, Vladimir Buchta 2, Martina Ceckova 1, Martin Dolezal 1, Frantisek Staud 1, Josef Jampilek 3 and Jarmila Kaustova 4 1 Faculty of Pharmacy in Hradec Kralove, Charles University in Prague, Heyrovskeho 1203, 500 05 Hradec Kralove, Czech Republic 2 Faculty of Medicine and University Hospital, Charles University in Prague, Sokolska 581, 500 05 Hradec Kralove , Czech Republic 3 Zentiva a.s., U Kabelovny 130, 102 37 Prague, Czech Republic 4 National Reference Laboratory for Mycobacterium kansasii, Regional Institute of Hygiene, 728 92 Ostrava, Czech Republic * Author to whom correspondence should be addressed; E-mail: jarmila.vinsova@faf.cuni.cz; Tel: (+420) 495 067 343; Fax: (+420) 495 514 330. Received: 27 October 2006; in revised form: 3 December 2006 / Accepted: 4 December 2004 / Published: 1 January 2007 Abstract: A new series of salicylanilide acetates was synthesized and evaluated for their in vitro antifungal and antituberculotic activity. Some of the evaluated compounds possessed comparable or better antifungal activity than a fluconazole standard. All these compounds exhibited very good potential and their in vitro activity against drug resistant and sensitive clinical isolates of Mycobacteria were found to be equivalent or better than a standard of isoniazide, a well-known first-line drug for tuberculosis treatment. Keywords: Salicylanilide acetates; in vitro antifungal activity; in vitro antimycobacterial activity; lipophilicity determination; cytotoxicity; structure-activity relationships. Introduction Salicylanilides possess a wide range of biological activities [1-4]. A new mechanism of action of these compounds was discovered in 1998. They act as inhibitors of the two-component regulatory system (TCS) in bacteria [5,6]. The importance of electron-