European Journal of Medicinal Chemistry ( IF 6.7 ) Pub Date : 2020-03-03 , DOI: 10.1016/j.ejmech.2020.112200 Steffan Willetts , David W. Foley
Aspirin is a widely used medicine for a variety of indications. It is unique amongst non-steroidal anti-inflammatory drugs (NSAIDs) in that it causes irreversible acetylation of COX enzymes. Like all NSAIDs however, aspirin causes severe gastrointestinal side-effects, in particular with chronic administration. Prodrugs of aspirin have been proposed as a solution to these side-effects. However, identifying true prodrugs of aspirin, rather than salicylic acid, has proven challenging. This review details the challenges and highlights recent progress in the development of such prodrugs.
中文翻译:
对或错?阿司匹林前药开发中的挑战和近期亮点
阿司匹林是用于各种适应症的广泛使用的药物。在非甾体类抗炎药(NSAID)中,它是独特的,因为它会导致COX酶的不可逆乙酰化。但是,像所有非甾体抗炎药一样,阿司匹林会引起严重的胃肠道副作用,尤其是长期服用时。已提出阿司匹林的前药作为这些副作用的解决方案。但是,事实证明,鉴定阿司匹林而不是水杨酸的真正前药具有挑战性。这篇综述详细介绍了挑战,并着重指出了此类前药开发的最新进展。