Salicylanilide esters of N-protected amino acids as novel antimicrobial agents
Salicylanilide esters of N-protected amino acids as novel antimicrobial agents
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DOI：
10.1016/j.bmcl.2008.11.080
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发表时间：
2009-01-15
影响因子：
2.7
通讯作者：
Jampilek, Josef
中科院分区：
文献类型：
--
作者：
Imramovsky, Ales;Vinsova, Jarmila;Jampilek, Josef
合成并表征了一系列新型的N-保护氨基酸水杨酰苯胺酯类化合物。测定了它们对8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、伞房犁头霉和须癣毛癣菌的活性最高，并且这些水平高于标准药物。氟康唑。此外，三个化合物显示出有趣的抗结核活性，抑制率为89%至99%。（S）-4-氯-2-（4-三氟甲基苯基氨基甲酰基）-苯基2-苄氧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。并对新化合物的构效关系进行了讨论。(C)2008爱思唯尔有限公司保留所有权利。
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. (C) 2008 Elsevier Ltd. All rights reserved.