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Synthesis and biological evaluation of novel benzothiazole clubbed fluoroquinolone derivatives

机译:新型苯并噻唑棒状氟喹诺酮衍生物的合成及生物评价

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Abstract In the present investigation, synthesis and anti-bacterial, analgesic and anthelmintic evaluation of a novel series of fluoroquinolone derivatives clubbed with benzothiazole moeity has been described. The synthesized compounds were characterised by spectral analysis (IR and 1H NMR). Preliminary results indicated that the most of the synthesized compounds demonstrated good activities against gram negative and gram positive bacterial strains. Compounds 5a, 5b, 5f and 5k demonstrated potent anti-bacterial activities. Compound 5a exhibited most potent anti-bacterial activity with MIC values of 04, 03, 08 and 15 μg/ mL against B. subtilis, S. aureus, E. coli and P. aeruginosa. Analogs 5a, 5c, 5g and 5h showed promising anthelmintic activity against Eisemia foetida in a low concentration as compared to standard drug piperazine citrate with mean paralysis time ranging 22.60?±?2.46 to 31.60?±?3.07?min. All synthesized compounds depicted good in vivo analgesic activity with compound 5a exhibiting the most potent activity of 55.19% inhibition of writhing in comparison to the standard drug.
机译:摘要在本研究中,已经描述了一系列新型苯并噻唑部分的氟喹诺酮衍生物的合成及抗菌,镇痛和驱虫评价。通过光谱分析(IR和 1 1H NMR)对合成的化合物进行表征。初步结果表明,大多数合成的化合物对革兰氏阴性和革兰氏阳性细菌菌株均表现出良好的活性。化合物5a,5b,5f和5k表现出强大的抗菌活性。化合物5a对枯草芽孢杆菌,金黄色葡萄球菌,大肠杆菌和铜绿假单胞菌具有最强的抗菌活性,MIC值为04、03、08和15μg/ mL。与标准药物枸pipe酸哌嗪相比,类似物5a,5c,5g和5h在低浓度下显示出对富血埃塞斯病的驱虫活性,其平均麻痹时间为22.60±2.46至31.60±3.07min。所有合成的化合物均表现出良好的体内止痛活性,与标准药物相比,化合物5a表现出最有效的55.19%扭体抑制活性。

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