新型肉桂碱融合曼尼希碱的合成:抗菌、镇痛和抗炎活性的药理评价

G. Kalyani, S. Bethi, K. V. Sastry, V. Kuchana
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引用次数: 4

摘要

本研究通过4-甲基-3-乙酰基肉桂啉与不同的仲芳香胺和脂肪胺缩合反应,设计并合成了一系列新型肉桂啉曼尼希碱,并用H1-NMR、IR和质谱对化合物的结构进行了表征。新合成的化合物对金黄色葡萄球菌(革兰氏阳性)和大肠杆菌(革兰氏阴性)的抑菌活性、体内镇痛和抗炎活性进行了生物学电位评价。与链霉素相比,化合物4和3具有较大的疏水氨基取代,对金黄色葡萄球菌和大肠杆菌的抗菌作用相对较高。同样,与双氯芬酸相比,化合物4在120分钟和180分钟的镇痛活性更高。从抗炎评估来看,与20 mg/kg剂量水平相比,50 mg/kg剂量水平的试验化合物报告了显著更高的活性。此外,与塞来昔布(20 mg/kg)相比,化合物4 (50 mg/kg)具有相似的抗炎活性。
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Synthesis of Novel Cinnoline Fused Mannich Bases: Pharmacological Evaluation of Antibacterial, Analgesic and Anti-Inflammatory Activities
In the present study, we have designed and synthesized a series of novel cinnoline fused Mannich bases by the condensation reaction of 4-methyl-3-acetyl cinnoline with different secondary aromatic and aliphatic amines with and the structures of compounds were characterized by H1-NMR, IR and Mass spectral analysis. The biological potentials of the newly synthesized compounds are evaluated for their antibacterial activity against Staphylococcus aureus (Gram positive), and Eeshricia coli (Gram negative) bacteria, in vivo analgesic and anti-inflammatory activities. Compounds 4 and 3, which are having larger hydrophobic amino substitutions resulted in relatively higher antibacterial against S. aureus and E. coli when compared to streptomycin. Similarly, compound 4 reported higher analgesic activity when compared to diclofenac at 120 mins and 180 mins. From anti-inflammatory evaluations, dose level of 50 mg/kg of test compounds reported significantly higher activity when compared to dose level of 20 mg/kg. Moreover, compound 4 (50 mg/kg) resulted in similar antiinflammatory activity when compared with celecoxib (20 mg/kg).
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