哌嗪取代喹唑啉基硫脲/噻唑烷酮/查尔酮复合物的合成及体外抗菌评价。

Bioorganicheskaia khimiia Pub Date : 2015-03-01
D R Shah, H P Lakum, K H Chikhalia
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引用次数: 0

摘要

在寻找新的生物实体来对抗最近的耐药微生物菌株的框架中,我们报告了一个基于喹唑啉的硫脲/4-噻唑烷酮/查尔酮杂交体文库。利用肉汤稀释技术研究了新合成的化合物对几种细菌(金黄色葡萄球菌、蜡样芽孢杆菌、铜绿假单胞菌和肺炎克雷伯菌)和真菌(白色念珠菌和棒状曲霉)的抑菌效果。生物学评价发现,(E)-3-(3,4-二甲氧基苯基)-1-(4-(4-(4-(4-乙基哌嗪-1-基)喹唑啉-2-基)氨基)苯基)prop-2-en-1-one对细菌生长的抑制作用最强(微生物抑制浓度为3.12 μg/mL)。其余化合物均具有与标准相同的药效(3.12 ~ 12.5 μg/mL)。最终化合物通过FT-IR、1H NMR、13C NMR、质谱和元素分析进行了表征。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
SYNTHESIS AND IN VITRO ANTIMICROBIAL EVALUATION OF PIPERAZINE SUBSTITUTED QUINAZOLINE-BASED THIOUREA/THIAZOLIDINONE/CHALCONE HYBRIDS.

In frames of the search for new biological entities to fight against recent drug-resistant microbial strains, we report a library of quinazoline-based thiourea/4-thiazolidinone/chalcone hybrids. The newly synthesized compounds were studied for efficacy against several bacteria (Staphylococcus aureus, Bacillus cereus, Pseudomonas aeruginosa, and Klebsiella pneumoniae) and fungi (Candida albicans and Aspergillus clavatus) using the broth dilution technique. From the biological evaluation, (E)-3-(3,4-dimethoxyphenyl)-1-(4-((4-(4-ethylpiperazin-1-yl)quinazolin-2-yl)amino)phenyl)prop-2-en-1-one was found to be the most active analogue (microbial inhibition concentration 3.12 μg/mL) to inhibit the bacterial growth. The rest of the compounds showed equipotent efficacy (3.12-12.5 μg/mL) as compared to the standard. Final compounds were characterized by FT-IR, 1H NMR, 13C NMR, mass spectroscopy, and elemental analysis.

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