一些非甾体抗炎药与肉桂醇形成的酯是具有增强抗炎活性的强效脂氧合酶抑制剂。

Esters of some non-steroidal anti-inflammatory drugs with cinnamyl alcohol are potent lipoxygenase inhibitors with enhanced anti-inflammatory activity.

作者信息

Theodosis-Nobelos Panagiotis, Kourti Malamati, Tziona Paraskevi, Kourounakis Panos N, Rekka Eleni A

机构信息

Department of Pharmaceutical Chemistry, School of Pharmacy, Aristotelian University of Thessaloniki, Thessaloniki 54124, Greece.

出版信息

Bioorg Med Chem Lett. 2015 Nov 15;25(22):5028-31. doi: 10.1016/j.bmcl.2015.10.036. Epub 2015 Oct 19.

DOI:10.1016/j.bmcl.2015.10.036

PMID:26494261

Abstract

Novel esters of non steroidal anti-inflammatory drugs, α-lipoic acid and indol-3-acetic acid with cinnamyl alcohol were synthesised by a straightforward method and at high yields (60-98%). They reduced acute inflammation more than the parent acids and are potent inhibitors of soybean lipoxygenase. Selected structures decreased plasma lipidemic indices in Triton-induced hyperlipidemia to rats. Therefore, the synthesised compounds may add to the current knowledge about agents acting against various inflammatory disorders.

摘要

通过一种简单的方法，以高产率（60-98%）合成了非甾体抗炎药、α-硫辛酸和吲哚-3-乙酸与肉桂醇的新型酯类。它们比母体酸更能减轻急性炎症，并且是大豆脂氧合酶的有效抑制剂。选定的结构可降低 Triton 诱导的大鼠高脂血症中的血浆脂质指标。因此，合成的化合物可能会增加目前关于对抗各种炎症性疾病的药物的知识。