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体外评价几种苯并咪唑衍生物作为抗氧化剂和黄嘌呤氧化酶抑制剂的活性。

In vitro evaluation of selected benzimidazole derivatives as an antioxidant and xanthine oxidase inhibitors.

机构信息

Department of Molecular Biotechnology, College of Life and Environmental Sciences, Konkuk University, Seoul, 143701, South Korea.

出版信息

Chem Biol Drug Des. 2013 Sep;82(3):290-5. doi: 10.1111/cbdd.12141. Epub 2013 Aug 9.

Abstract

2-Aryl-1-arylmethyl-1H-benzimidazole derivatives having different side chains on the structure were examined in vitro for their antioxidant abilities by 2,2-diphenyl-1-picryl hydrazine radical scavenging activity, reducing ability, OH radical scavenging activity, inhibition of polyphenol oxidase and xanthine oxidase. Overall, with few exceptions, all the 2-aryl-1-arylmethyl-1H-benzimidazoles showed moderate biological activity with all parameters examined. The 2-aryl-1-arylmethyl-1H-benzimidazoles were found to be reactive toward 2,2-diphenyl-1-picryl hydrazine radical and had considerable reducing ability, with significant xanthine oxidase inhibition. With few exceptions, all the compounds under study were found to possess moderate-to-poor OH radical scavenging activity and inhibited polyphenol oxidase significantly. These findings suggest that these 2-aryl-1-arylmethyl-1H-benzimidazoles can be considered as potential antioxidant and xanthine oxidase inhibitory agents, those might be further, explored for the design of lead antioxidant and antigout drug candidates using in vivo trials.

摘要

2-芳基-1-芳甲基-1H-苯并咪唑衍生物在结构上具有不同的侧链,通过 2,2-二苯基-1-苦基肼自由基清除活性、还原能力、OH 自由基清除活性、对多酚氧化酶和黄嘌呤氧化酶的抑制作用,对其体外抗氧化能力进行了研究。总体而言,除了少数例外,所有的 2-芳基-1-芳甲基-1H-苯并咪唑都表现出中等的生物活性,所有参数都得到了检测。研究发现,2-芳基-1-芳甲基-1H-苯并咪唑对 2,2-二苯基-1-苦基肼自由基具有反应活性,具有相当的还原能力,对黄嘌呤氧化酶有显著的抑制作用。除了少数例外,所有研究的化合物都具有中等至较差的 OH 自由基清除活性,并显著抑制多酚氧化酶。这些发现表明,这些 2-芳基-1-芳甲基-1H-苯并咪唑可以被认为是潜在的抗氧化剂和黄嘌呤氧化酶抑制剂,这些化合物可能会进一步通过体内试验来探索设计用于抗氧化和抗痛风的先导药物候选物。

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