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Nonsteroidal Anti-Inflammatory Drugs (NSAIDs): Progress in Small Molecule Drug Development

机译:非甾体抗炎药(NSAIDs):小分子药物开发的进展

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摘要

Ever since the discovery of aspirin, small molecule therapeutics have been widely prescribed to treat inflammation and pain. Aspirin and several small molecule NSAIDs are known to inhibit the enzymes cyclooxygenase-1 (COX-1) and -2 (COX-2). Despite the success of NSAIDs to treat inflammatory disorders, the development of a clinically useful small molecule NSAIDs with decreased side effect profiles is an ongoing effort. The recent discovery and development of selective COX-2 inhibitors was a step toward this direction. Emerging trends are represented by the progress in the development of hybrid agents such as nitric oxide donor-NSAIDs (NO-NSAIDs) and dual COX/lipoxygenase (LOX) inhibitors. This review focuses on the recent advances in the rational design of small molecule NSAIDs in therapy.
机译:自发现阿司匹林以来,小分子疗法已被广泛指定用于治疗炎症和疼痛。已知阿司匹林和几种小分子非甾体抗炎药会抑制环氧合酶-1(COX-1)和-2(COX-2)酶。尽管NSAIDs治疗炎症性疾病成功,但是正在开发具有降低的副作用特征的临床上有用的小分子NSAIDs。选择性COX-2抑制剂的最新发现和开发是朝这个方向迈出的一步。新兴趋势以诸如一氧化氮供体-NSAIDs(NO-NSAIDs)和双重COX /脂氧合酶(LOX)抑制剂等杂合剂的开发进展为代表。这篇综述着重于小分子NSAID在治疗中的合理设计方面的最新进展。

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