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首页> 外文期刊>Medicinal chemistry >Synthesis, Anticonvulsant and Antimicrobial Activities of Some New [1-(2-Naphthyl)-2-(pyrazol-1-yl)ethanone]oxime Ethers
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Synthesis, Anticonvulsant and Antimicrobial Activities of Some New [1-(2-Naphthyl)-2-(pyrazol-1-yl)ethanone]oxime Ethers

机译:一些新型[1-(2-萘基)-2-(吡唑-1-基)乙酮]肟醚的合成,抗惊厥和抑菌活性

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摘要

In this study, 12 new oxime ether derivatives, which were expected to show anticonvulsant and antimicrobial activities, were synthesized. Oxime ether derivatives were synthesized by the reaction of various alkyl halides with 1-(2-naphthyl)- 2-(pyrazol-1-yl)ethanone oxime. Anticonvulsant activity of the compounds was determined by maximal electroshock (MES) and subcutaneous metrazol (ScM) seizure tests, while neurological disorders were evaluated using rotorod toxicity test according to the ASP of NIH. Compound 1, 6 and 7 showed anticonvulsant activity at 300 mg/kg dose at 4 h, but compounds 1 and 7 showed toxicity at 300 mg/kg dose at half an hour. Antimicrobial activities of the compounds were also determined using agar microdilution method. Compound 1 and 5 were found to have the highest antifungal activity among the other compounds.
机译:在这项研究中,合成了12种新的肟醚衍生物,这些衍生物预期具有抗惊厥和抗菌活性。通过各种烷基卤与1-(2-萘基)-2-(吡唑-1-基)乙酮肟的反应合成肟醚衍生物。通过最大电击(MES)和皮下甲硝唑(ScM)癫痫发作试验确定化合物的抗惊厥活性,同时根据NIH的ASP使用旋翼毒性试验评估神经系统疾病。化合物1、6和7在4小时以300mg / kg的剂量显示出抗惊厥活性,但是化合物1和7在半小时以300mg / kg的剂量显示出毒性。还使用琼脂微稀释法确定化合物的抗菌活性。发现化合物1和5在其他化合物中具有最高的抗真菌活性。

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