N-保护氨基酸的水杨酰苯胺酯作为新型抗菌剂。
Salicylanilide esters of N-protected amino acids as novel antimicrobial agents.
作者信息
Imramovský Ales, Vinsová Jarmila, Férriz Juana Monreal, Buchta Vladimír, Jampílek Josef
机构信息
Department of Inorganic and Organic Chemistry, Faculty of Pharmacy, Charles University, Heyrovskeho 1203, 500 05 Hradec Kralove, Czech Republic.
出版信息
Bioorg Med Chem Lett. 2009 Jan 15;19(2):348-51. doi: 10.1016/j.bmcl.2008.11.080. Epub 2008 Nov 27.
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.
合成并表征了一系列新型的、具有高抗菌活性的N-保护氨基酸水杨酰苯胺酯。测定了它们对八种真菌菌株和结核分枝杆菌的体外抗菌活性。这些化合物对烟曲霉、伞枝犁头霉和须癣毛癣菌具有最高水平的活性，且这些水平高于标准药物氟康唑。此外，三种化合物表现出有趣的抗结核活性，抑制率在89%至99%之间。(S)-4-氯-2-(4-三氟甲基苯基氨基甲酰基)-苯基2-苄氧基羰基氨基丙酸酯具有最高水平的抗真菌和抗分枝杆菌活性。讨论了新化合物的构效关系。
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