水杨醛类多齿席夫碱的合成、表征及抗菌活性研究

Yosef Bayeh, Fekiya Mohammed, Mamo Gebrezgiabher, Fikre Elemo, Mesfin Getachew, Madhu Thomas
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引用次数: 4

摘要

通过水杨醛与4-氨基安替比林、乙二胺和2-氨基苯酚的缩合反应,合成了三种席夫碱L1、L2和L3,并通过各种物理化学研究对其进行了表征。用琼脂扩散法筛选三种化合物对金黄色葡萄球菌(S.A)、表皮葡萄球菌(S.E)、肺炎克雷伯菌(K.P)和绿脓杆菌(P.A)两种革兰氏阴性菌的抗菌活性。将获得的结果与市售抗生素如环丙沙星和氯霉素的活性进行比较,新合成的化合物显示出相当的抗菌活性。溶剂甲醇对所有细菌的活性范围为8±0.25至17±0.29mm,而标准抗生素环丙沙星和氯霉素的活性范围分别为21.3±0.31至28.3±0.32和26.3±0.24mm至32.3±0.23mm。然而,新合成的席夫碱L1、L2和L3的IZ分别为7.4±0.23至32.5±0.14、3±0.57至12±0.28和10±0.20至32±0.36。在希夫碱中,L3对S.E和P.A的活性为(32±0.36),高于标准抗生素环丙沙星和氯霉素对相同菌株的活性。结果表明,经过进一步的体内细胞毒性研究,所有合成的希夫碱对所有可能产生希夫碱的细菌都表现出明显的抗菌活性,可作为广泛的抗菌药物应用。它们的活性还可以通过改变席夫碱缩合前体的官能度来进一步修饰。
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Synthesis, Characterization and Antibacterial Activities of Polydentate Schiff Bases, Based on Salicylaldehyde
Three Schiff bases L1, L2 and L3 were synthesized by condensing salicylaldehyde with 4-aminoantipyrine, ethylendiamine and 2-aminophenol respectively and subsequently characterized by various physicochemical investigations. All the three compounds were screened for their In-vitro antibacterial activity against two gram positive bacteria, Staphylococcus aureus (S.A), Staphylococcus epidermidis (S.E) and two gram negative bacteria Klebsiella pneumoniae (K.P) and Pseudomonas aeruginosa (P.A) by agar diffusion method. On comparing the results obtained with the activity of commercially available antibiotics such as Ciprofloxacin and Chloramphenicol, the newly synthesized compounds showed comparable antibacterial activities. The solvent methanol exhibit activity against all bacterial species with IZs ranging from 8 ± 0.25 to 17 ± 0.29 mm while the standard antibiotics Ciprofloxacin and Chloramphenicol exhibited an activities with IZs varying from 21.3 ± 0.31 to 28.3 ± 0.32 and 26.3 ± 0.24 mm to 32.3 ± 0.23 mm, respectively. However, the newly synthesized Schiff bases L1, L2 and L3 showed IZs ranging from 7.4 ± 0.23 to 32.5 ± 0.14, 3 ± 0.57 to 12 ± 0.28 and 10 ± 0.20 to 32 ± 0.36 respectively. Among the Schiff bases, L3 showed the activity (32 ± 0.36) against S.E and P.A which is higher than the activity of standard antibiotics Ciprofloxacin and Chloramphenicol against the same bacterial strains. The results obtained revealed that all the synthesized Schiff bases exhibit appreciable antibacterial activity against all the bacteria species which potentially makes them, to apply as wide range antibacterial drugs, after further in-vivo cytotoxicity investigations. Their activity can also be further modified by changing the functionality of precursors for Schiff base condensation.
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