Ziakas George N, Rekka Eleni A, Gavalas Antonios M, Eleftheriou Phaedra T, Kourounakis Panos N
Department of Pharmaceutical Chemistry, School of Pharmacy, Aristotelian University of Thessaloniki, Greece.
Bioorg Med Chem. 2006 Aug 15;14(16):5616-24. doi: 10.1016/j.bmc.2006.04.030. Epub 2006 May 11.
Amine or amide derivatives bearing the 2,6-di-tert-butyl phenol moiety are synthesised. Almost all are antioxidants, reduce acute inflammation and inhibit COX-1 and lipoxygenase activity. The most potent anti-inflammatory, COX-1 inhibitor and antioxidant agent, with low toxicity, is 2,6-di-tert-butyl-4-thiomorpholin-4-ylmethyl-phenol.
合成了带有2,6-二叔丁基苯酚部分的胺或酰胺衍生物。几乎所有这些衍生物都是抗氧化剂，能减轻急性炎症并抑制COX-1和脂氧合酶的活性。最有效的抗炎、COX-1抑制剂和抗氧化剂，且毒性较低的是2,6-二叔丁基-4-硫代吗啉-4-基甲基苯酚。
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