具有抗炎活性且胃肠道安全性良好的释放一氧化氮的托芬那酸衍生物。
Nitric oxide releasing derivatives of tolfenamic acid with anti-inflammatory activity and safe gastrointestinal profile.
作者信息
Ziakas George N, Rekka Eleni A, Gavalas Antonios M, Eleftheriou Phaedra T, Tsiakitzis Karyofillis C, Kourounakis Panos N
机构信息
Department of Pharmaceutical Chemistry, School of Pharmacy, Aristotelian University of Thessaloniki, Greece.
出版信息
Bioorg Med Chem. 2005 Dec 1;13(23):6485-92. doi: 10.1016/j.bmc.2005.07.049. Epub 2005 Sep 26.
Tolfenamic acid esters with nitrooxyalcohols are synthesized. They are anti-inflammatory agents reducing carrageenan rat paw edema, with low gastrointestinal and general toxicity. In vitro, they are nitric oxide donors, inhibitors of lipoxygenase and cyclooxygenases. A two to three carbon chain between carboxylic and nitric ester groups seems optimal for activity.
合成了托芬那酸与硝基氧基醇的酯类化合物。它们是抗炎剂，可减轻角叉菜胶所致大鼠足爪水肿，且具有低胃肠道毒性和全身毒性。在体外，它们是一氧化氮供体、脂氧合酶和环氧化酶的抑制剂。羧酸酯基和硝酸酯基之间具有两到三个碳原子的链似乎对活性最为有利。
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