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Synthesis, characterization, and quantitative structure-activity relationship studies of bioactive dehydroacetic acid and amino ether Schiff base complexes
Heteroatom Chemistry ( IF 0.3 ) Pub Date : 2016-09-09 , DOI: 10.1002/hc.21347
Jai Devi 1 , Suman Devi 1 , Ashwani Kumar 2
Affiliation  

Structural aspects of organosilicon(IV) and organotin(IV) complexes with dehydroacetic acid and amino ether Schiff base ligand have been described with the help of elemental analyses, conductance measurements, UV–Vis, infrared, multinuclear magnetic resonance, mass spectroscopy as well as thermogravimetric analysis, and X-ray diffraction studies. Analysis of data suggested that the Schiff base provides two bidentate NO domains and was coordinated to silicon and tin moiety through the imine nitrogen and hydroxyl oxygen atom. Complexes were found to be nonelectrolytic and monomeric in nature. The thermal decomposition for tin compounds occurred in two steps and resulted into the formation of pure SnO2 as end product. The in vitro biological effects of the synthesized compounds were tested against two Gram-positive and two Gram-negative bacteria. The results of biological activity showed that all the complexes have enhanced activity as compared with the corresponding ligand, and compounds 5, 9, 11, 12, 13, 15, 16, and 17 were more potent than the standard drug ciprofloxacin. Compound 17 exhibited best antibacterial activity with lowest minimum inhibitory concentration value and maximum zone of inhibition. Further, quantitative structure–activity relationship studies pointed out that more stable compound were more active as antibacterial agents.

中文翻译:

生物活性脱氢乙酸和氨基醚席夫碱配合物的合成、表征和定量构效关系研究

有机硅 (IV) 和有机锡 (IV) 与脱氢乙酸和氨基醚席夫碱配体的配合物的结构方面已经在元素分析、电导测量、紫外-可见、红外、多核磁共振、质谱以及质谱的帮助下进行了描述热重分析和 X 射线衍射研究。数据分析表明,席夫碱提供了两个双齿 NO 结构域,并通过亚胺氮和羟基氧原子与硅和锡部分配位。发现配合物本质上是非电解的和单体的。锡化合物的热分解分两步进行,最终形成纯 SnO2。针对两种革兰氏阳性菌和两种革兰氏阴性菌测试了合成化合物的体外生物学效应。生物活性结果表明,与相应的配体相比,所有配合物均具有增强的活性,化合物5、9、11、12、13、15、16和17比标准药物环丙沙星更有效。化合物17表现出最好的抗菌活性,最低抑菌浓度值最低,抑菌圈最大。此外,定量构效关系研究指出,更稳定的化合物作为抗菌剂的活性更高。化合物17表现出最好的抗菌活性,最低抑菌浓度值最低,抑菌圈最大。此外,定量构效关系研究指出,更稳定的化合物作为抗菌剂的活性更高。化合物17表现出最好的抗菌活性,最低抑菌浓度值最低,抑菌圈最大。此外,定量构效关系研究指出,更稳定的化合物作为抗菌剂的活性更高。
更新日期:2016-09-09
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