Salicylanilide esters of N-protected amino acids as novel antimicrobial agents |
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| Authors: | Ale? Imramovský Jarmila Vin?ová Juana Monreal Férriz Vladimír Buchta Josef Jampílek |
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| Institution: | 1. Department of Inorganic and Organic Chemistry, Faculty of Pharmacy, Charles University, Heyrovskeho 1203, 500 05 Hradec Kralove, Czech Republic;2. Institute of Organic Chemistry and Technology, Faculty of Chemical Technology, University of Pardubice, nam. Cs. Legii 565, 532 10 Pardubice, Czech Republic;3. Faculty of Medicine and University Hospital, Charles University, Sokolska 581, 500 05 Hradec Kralove, Czech Republic;4. Zentiva a.s., U kabelovny 130, 102 37 Prague, Czech Republic;5. Department of Chemical Drugs, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences, Palackeho 1/3, 612 42 Brno, Czech Republic |
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| Abstract: | A series of novel, highly antimicrobial salicylanilide esters of N-protected amino acids were synthesized and characterized. Their in vitro antimicrobial activity against eight fungal strains and Mycobacterium tuberculosis was determined. The compounds had the highest level of activity against Aspergillus fumigatus, Absidia corymbifera and Trichophyton mentagrophytes, and these levels were higher than that of the standard drug fluconazole. In addition, three compounds showed interesting antituberculosis activity, with inhibition ranging from 89% to 99%. (S)-4-Chloro-2-(4-trifluoromethylphenylcarbamoyl)-phenyl 2-benzyloxy-carbonylamino-propionate had the highest level of both antifungal and antimycobacterial activity. The structure–activity relationships of the new compounds are discussed. |
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