取代苯并咪唑衍生物的合成及抗氧化活性评价

Shejuti Rahman Brishty, Poushali Saha, Z. A. Mahmud, S. Rahman
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引用次数: 6

摘要

本研究以铵盐为催化剂,通过不同的邻芳基二胺化合物与相应的醛缩合,合成了以3A-1、3A-2、3A-3、3B-1和3B-2命名的取代苯并咪唑衍生物,并对其进行了药理学评价。所有化合物均通过红外光谱和核磁共振光谱进行了表征。采用醋酸扭体抑制法和DPPH自由基清除法研究合成的苯并咪唑衍生物对瑞士白化小鼠的镇痛和抗氧化活性。化合物3A-3、3B-1和3B-2在50 mg/kg体重剂量下与标准双氯芬酸(90.76%)相比,分别减少了88.24%、84.03%和85.71%的扭体次数(p<0.001)。与标准丁基羟基甲苯(BHT) (14.44 μg/ml)相比,3A-1、3A-2、3A-3和3B-2的IC50分别为0.038、0.959、8.834和7.519 μg/ml,具有较强的抗氧化活性。在合成的化合物中,3A-3和3B2被认为是最有前途的镇痛和抗氧化剂,并有望成为未来研究的先导化合物。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Synthesis and Evaluation of Analgesic and Antioxidant Activities of Substituted Benzimidazole Derivatives
The present study describes the synthesis and pharmacological evaluation of a number of substituted benzimidazole derivatives designated by 3A-1, 3A-2, 3A-3, 3B-1 and 3B-2 through condensation of different o-aryldiamine compounds with the corresponding aldehyde employing ammonium salt as a catalyst. All the compounds were characterized by IR and H NMR spectroscopic analysis. The synthesized benzimidazole derivatives were investigated for analgesic and antioxidant activities using acetic acid-induced writhing inhibition in Swiss albino mice and DPPH free radical scavenging assay, respectively. Compounds 3A-3, 3B-1 and 3B-2 at a dose of 50 mg/kg body weight reduced the number of writhings by 88.24%, 84.03% and 85.71%, respectively (p<0.001) in comparison with standard diclofenac (90.76% inhibition). The derivatives 3A-1, 3A-2, 3A-3 and 3B-2 showed prominent antioxidant activity with IC50 values of 0.038, 0.959, 8.834 and 7.519 μg/ml, respectively in comparison with the standard butylated hydroxytoluene (BHT) (14.44 μg/ml). Among the synthesized compounds, 3A-3 and 3B2 emerged as the most promising analgesic and antioxidant agents and expressed their potential as lead compounds in future research.
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