Salicylanilide carbamates: Antitubercular agents active against multidrug-resistant Mycobacterium tuberculosis strains |
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| Authors: | Juana M. Férriz Kateřina Vávrová Filip Kunc Aleš Imramovský Jiřina Stolaříková Eva Vavříková Jarmila Vinšová |
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| Affiliation: | 1. Charles University, Faculty of Pharmacy, Department of Inorganic and Organic Chemistry, Heyrovského 1203, 500 05 Hradec Králové, Czech Republic;2. Charles University, Faculty of Medicine in Hradec Králové, Department of Medicinal Biology, ?imkova 870, 500 38 Hradec Králové, Czech Republic;3. Generi Biotech, Machkova 587, 500 11 Hradec Králové, Czech Republic;4. Institute of Organic Chemistry and Technology, Faculty of Chemistry and Chemical Technology, University of Pardubice, Studentská 573, 532 10 Pardubice, Czech Republic;5. Laboratory for TBC, Health Institute in Ostrava, 702 00 Ostrava, Czech Republic |
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| Abstract: | A series of 27 salicylanilide-based carbamates was prepared as a part of our ongoing search for new antituberculosis drugs. These compounds exhibited very good in vitro activity against Mycobacterium tuberculosis, Mycobacterium kansasii and Mycobacterium avium and, in particular, against five multidrug-resistant strains, with MIC values between 0.5–2 μmol/L. Moreover, they displayed moderate toxicity against intestinal cells with the selectivity index being up to 96. Furthermore, acid stability and a half-life of 43 h at pH 7.4 were shown. Thus, these novel salicylanilide derivatives are drug candidates which should be seriously consider for further screening. |
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