阿司匹林新型一氧化氮供体型酯类的抗炎、保护胃黏膜及抗血小板特性。
Antiinflammatory, gastrosparing, and antiplatelet properties of new NO-donor esters of aspirin.
作者信息
Cena Clara, Lolli Marco L, Lazzarato Loretta, Guaita Elena, Morini Giuseppina, Coruzzi Gabriella, McElroy Stuart P, Megson Ian L, Fruttero Roberta, Gasco Alberto
机构信息
Dipartimento di Scienza e Tecnologia del Farmaco, Università degli Studi di Torino, via Pietro Giuria 9, 10125 Torino, Italy.
出版信息
J Med Chem. 2003 Feb 27;46(5):747-54. doi: 10.1021/jm020969t.
A new series of NSAIDs in which aspirin is joined by an ester linkage to furoxan moieties, with different ability to release NO, were synthesized and tested for NO-releasing, antiinflammatory, antiaggregatory, and ulcerogenic properties. Related furazan derivatives, aspirin, its propyl ester, and its gamma-nitrooxypropyl ester were taken as references. All the products described present an antiinflammatory trend, maximized in derivatives 12, 16, and 17, they are devoid of acute gastrotoxicity, principally due to their ester nature, and show an antiplatelet activity primarily determined by their ability to release NO. They do not behave as aspirin prodrugs in human serum.
合成了一系列新的非甾体抗炎药，其中阿司匹林通过酯键与呋咱部分相连，具有不同的释放一氧化氮（NO）的能力，并对其释放NO、抗炎、抗聚集和致溃疡特性进行了测试。相关的呋咱衍生物、阿司匹林、其丙酯及其γ-硝基氧丙酯作为参考。所描述的所有产品都呈现出抗炎趋势，在衍生物12、16和17中达到最大值，它们没有急性胃毒性，主要归因于其酯的性质，并且显示出主要由其释放NO的能力决定的抗血小板活性。它们在人血清中不作为阿司匹林前药起作用。
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