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Synthesis, antibacterial evaluation, in silico ADMET and molecular docking studies of new N-acylhydrazone derivatives from acridone
Arabian Journal of Chemistry ( IF 6 ) Pub Date : 2020-07-01 , DOI: 10.1016/j.arabjc.2020.05.034
Mohammed Aarjane , Adnane Aouidate , Siham Slassi , Amina Amine

Abstract Novel N-acylhydrazone derivatives from acridone have been synthesized by condensation of acridone acetohydrazide and various aldehyde. The novel acylhydrazones were tested for their in-vitro antibacterial activity against human pathogenic strains. The MIC results indicate that compound 3f displayed high antibacterial potential against Pseudomonas putida with MIC = 38.46 µg/mL, which is very close to that obtained with the commercial antibiotic. The synthesized compounds were subjected for docking studies to understand the interaction of our compounds and transcriptional regulator enzyme of pseudomonas putida and DNA gyrase complex of Staphyloccocus aureus.

中文翻译:

来自吖啶酮的新型 N-酰基腙衍生物的合成、抗菌评价、计算机模拟 ADMET 和分子对接研究

摘要 通过吖啶酮乙酰肼与各种醛缩合合成了新型的吖啶酮N-酰基腙衍生物。测试了新型酰基腙对人类致病菌株的体外抗菌活性。MIC 结果表明,化合物 3f 对恶臭假单胞菌表现出很高的抗菌潜力,MIC = 38.46 µg/mL,与商业抗生素获得的结果非常接近。对合成的化合物进行对接研究,以了解我们的化合物与恶臭假单胞菌转录调节酶和金黄色葡萄球菌 DNA 促旋酶复合物的相互作用。
更新日期:2020-07-01
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