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Synthesis and Biological Evaluation of (E)-N’-Benzylidene-7-methyl-2-propyl-1H-benzo[d] imidazole-5-carbohydrazides as Antioxidant, Anti-inflammatory and Analgesic agents
Heterocyclic Communications ( IF 1.3 ) Pub Date : 2019-04-03 , DOI: 10.1515/hc-2019-0009
Ramamurthy Katikireddy 1 , Ramu Kakkerla 2 , M. P. S. Murali Krishna 3 , Gandamalla Durgaiah 4 , Y. N. Reddy 4 , Mavurapu Satyanarayana 5
Affiliation  

Abstract (E)-N’-Benzylidene-7-methyl-2-propyl-1H-benzo [d]imidazole-5-carbohydrazides (5a-r) have been synthesized from 7-methyl-2-propyl-1H-benzo[d]imidazole-5-carbohydrazide (3) by condensing with different aromatic aldehydes (4a-r). Title compounds (5a-r) were evaluated for in vitro antioxidant activity and based on their potential for antioxidant property, selected compounds 5d and 5m-p were screened for in vivo anti-inflammatory and analgesic activity. The results indicate that the compound 5o and 5p are effective against anti-inflammatory and analgesic activity. The biological data was further supported by molecular docking studies, which revealed the binding pattern and the affinity of the molecules in the active site of COX-2.

中文翻译:

(E)-N'-Benzylidene-7-methyl-2-propyl-1H-benzo[d] imidazole-5-carbohydrazides 作为抗氧化剂、抗炎剂和镇痛剂的合成和生物学评价

摘要 (E)-N'-苯亚甲基-7-甲基-2-丙基-1H-苯并[d]咪唑-5-碳酰肼(5a-r)由7-甲基-2-丙基-1H-苯并[d]咪唑-5-碳酰肼(5a-r)合成。 d]imidazole-5-carbohydrazide (3) 通过与不同的芳香醛 (4a-r) 缩合。对标题化合物 (5a-r) 的体外抗氧化活性进行了评估,并根据它们的抗氧化性能潜力,筛选出所选化合物 5d 和 5m-p 的体内抗炎和镇痛活性。结果表明化合物5o和5p对抗炎和镇痛活性有效。分子对接研究进一步支持了生物学数据,该研究揭示了 COX-2 活性位点中分子的结合模式和亲和力。
更新日期:2019-04-03
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