4-(2-氨基苯基)吗啉席夫碱的合成与药理评价

Synthesis and pharmacological evaluation of schiff bases of 4-(2-aminophenyl)-morpholines.

作者信息

Panneerselvam P, Priya M Gnanarupa, Kumar N Ramesh, Saravanan G

机构信息

Department of Pharmaceutical Chemistry, C. L. Baid Mehta College of Pharmacy, Jyothi Nagar, Old Mahabaliupuram Road, Thoraipakkam, Chennai-600 096, India.

出版信息

Indian J Pharm Sci. 2009 Jul;71(4):428-32. doi: 10.4103/0250-474X.57292.

DOI:10.4103/0250-474X.57292

PMID:20502549

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2865815/

Abstract

In the present study, a novel series of 4-(2-aminophenyl)morpholines were synthesized and characterized by IR, (1)H-NMR, (13)C NMR and mass spectral analysis. The synthesized compounds were screened for analgesic (100 and 200 mg/kg), antiinflammatory (200 and 400 mg/kg), antibacterial (Bacillus subtilis, Bacillus cereus, Staphylococcus epidermidis, Staphylococcus aureus, Klebsiella pneumoniae, Pseudomonas aeruginosa and Escherichia coli) and antifungal (Candida albicans and Aspergillus niger) activities. The minimum inhibitory concentrations of the compounds were also ascertained by agar streak dilution method. N-benzylidine-2-morpholoino benzenamine (1) and N-(3-nitro benzylidine)-2-morpholino benzenamine (3) exhibited significant analgesic, antiinflammatory and antimicrobial activities.

摘要

在本研究中，合成了一系列新型的4-(2-氨基苯基)吗啉，并通过红外光谱、¹H-NMR、¹³C NMR和质谱分析对其进行了表征。对合成的化合物进行了镇痛（100和200mg/kg）、抗炎（200和400mg/kg）、抗菌（枯草芽孢杆菌、蜡样芽孢杆菌、表皮葡萄球菌、金黄色葡萄球菌、肺炎克雷伯菌、铜绿假单胞菌和大肠杆菌）和抗真菌（白色念珠菌和黑曲霉）活性筛选。还通过琼脂划线稀释法确定了化合物的最低抑菌浓度。N-苄叉基-2-吗啉基苯甲胺（1）和N-(3-硝基苄叉基)-2-吗啉基苯甲胺（3）表现出显著的镇痛、抗炎和抗菌活性。