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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >New quinoline derivatives: synthesis and investigation of antibacterial and antituberculosis properties.
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New quinoline derivatives: synthesis and investigation of antibacterial and antituberculosis properties.

机译：新喹啉衍生物：抗菌和抗结核特性的合成和研究。

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Four new series of quinoline derivatives were synthesized starting from 2-trifluoromethyl aniline through multi-step reactions. In the reaction sequence, substituted aniline was cyclized to 4-hydroxy quinoline 1, which was then transformed to 4-chloro-2,8-bis(trifluoromethyl)quinoline 2. The key scaffold 4-hydrazinyl-2,8-bis(trifluoromethyl)quinoline 3, obtained from the compound 2, was successfully converted to target quinoline derivatives, viz. hydrazones 4a-t, ureas 5a-e, thioureas 6a-c and pyrazoles 7a-d, in good yields. The newly synthesized title compounds were evaluated for their in vitro antibacterial activity against Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa and Klebsiella pneumoniae (recultured) and antituberculosis activity against Mycobacterium tuberculosis H(37)Rv and MDR-TB. Preliminary results indicated that most of the hydrazone derivatives demonstrated very good antibacterial and antituberculosis activities while other derivatives showed moderate activity.
机译：从2-三氟甲基苯胺开始，通过多步反应合成了四个新系列的喹啉衍生物。在反应顺序中，将取代的苯胺环化为4-羟基喹啉1，然后将其转化为4-氯-2,8-双（三氟甲基）喹啉2。关键支架4-肼基-2,8-双（三氟甲基）将从化合物2获得的）喹啉3成功转化为目标喹啉衍生物，即。 good 4a-t，脲5a-e，硫脲6a-c和吡唑7a-d，收率良好。评价了新合成的标题化合物对大肠杆菌，金黄色葡萄球菌，铜绿假单胞菌和肺炎克雷伯菌的体外抗菌活性（再培养）以及对结核分枝杆菌H（37）Rv和MDR-TB的抗结核活性。初步结果表明，大多数derivatives衍生物表现出非常好的抗菌和抗结核活性，而其他衍生物则表现出中等的活性。

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