Synthesis, In vitro Antibacterial and Antifungal Activities of Trifluoroalkyl-N, N’-Disubstituted Thioureas

M. Sanhoury
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引用次数: 2

Abstract

A series of N-(4-trifluoromethylphenyl) thiourea derivatives of biological interest has been prepared by the condensation of various isothiocyanates with primary 4-trifluorophenylamine under uncatalyzed conditions. The chemical structures of all the reported compounds were confirmed by FT-IR, multinuclear NMR (1H, 13C, 19F) and HRMS spectrometry. Some of these compounds were screened for their in vitro antibacterial activity against ten pathogenic strains representing different types of gram-positive and gram-negative bacteria, two pathogenic fungi ( Penicilluim sp, Aspergillus flavus ) and two yeasts ( Candida albicans and Candida glabrata ). More than four of the synthesized compounds showed promising inhibition activities against the tested strains ATCC 19436 with reference to standard vancomycin. Best antimicrobial activity was founded for the 3-pyridylthiourea derivative against Enterococcus faecuim ATCC 25923 with CMI= 3.9 mg/mL. The results indicated also that all the new screened compounds have promising antifungal activity comparable to the activity observed for the reference compounds.
三氟烷基-N, N ' -二取代硫脲的合成及体外抑菌活性研究
在非催化条件下,用不同的异硫氰酸酯与伯4-三氟苯胺缩合制备了一系列具有生物学意义的N-(4-三氟甲基苯基)硫脲衍生物。所有化合物的化学结构均通过FT-IR、多核磁共振(1H, 13C, 19F)和HRMS谱分析得到证实。部分化合物对10种不同类型的革兰氏阳性菌和革兰氏阴性菌、2种病原真菌(青霉、黄曲霉)和2种酵母菌(白色念珠菌和面露念珠菌)的体外抗菌活性进行了筛选。以标准万古霉素为对照,有4个以上化合物对ATCC 19436具有良好的抑制活性。3-吡啶硫脲衍生物对粪肠球菌ATCC 25923的抑菌活性最佳,CMI= 3.9 mg/mL。结果还表明,所有新筛选的化合物都具有与参比化合物相当的抗真菌活性。
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