Benzimidazole derivatives: search for GI-friendly anti-inflammatory analgesic agents

苯并咪唑衍生物:寻找胃肠道友好的抗炎镇痛药

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作者:Monika Gaba, Punam Gaba, Deepika Uppal, Neelima Dhingra, Malkeet Singh Bahia, Om Silakari, Chander Mohan

Abstract

Non-steroidal anti-inflammatory drugs (NSAIDs) have been successfully used for the alleviation of pain and inflammation in the past and continue to be used daily by millions of patients worldwide. However, gastrointestinal (GI) toxicity associated with NSAIDs is an important medical and socioeconomic problem. Local generation of various reactive oxygen species plays a significant role in the formation of gastric ulceration associated with NSAIDs therapy. Co-medication of antioxidants along with NSAIDs has been found to be beneficial in the prevention of GI injury. This paper describes the synthesis and biological evaluation of N-1-(phenylsulfonyl)-2-methylamino-substituted-1H-benzimidazole derivatives as anti-inflammatory analgesic agents with lower GI toxicity. Studies in vitro and in vivo demonstrated that the antioxidant activity of the test compounds decreased GI toxicity.

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