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

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• 作者：Panagiotis Theodosis-Nobelos ; Malamati Kourti ; Paraskevi Tziona ; Panos N. Kourounakis ; Eleni A. Rekka ; ^{rekka@pharm.auth.gr" class="auth_mail" title="E-mail the corresponding author}
• 关键词：LVLBUSIGJCVSDD-RMKNXTFCSA-N ; KZTKNDJVKFBRLC-RMKNXTFCSA-N ; SPJHTGMQFLFYQG-JXMROGBWSA-N ; YQDCBKOZTABFIV-FMIVXFBMSA-N ; HXOONHWKCIBQAF-RMKNXTFCSA-N ; LYLQYJYCLOSVOA-RMKNXTFCSA-N ; HKQWGQKRXXFZLY-JXMROGBWSA-N ; VFHJKTCIDHWSKH-DHZHZOJOSA-N ; OAGBLSUDLZZXKV-JXMROGBWSA-N ; OIMWPABFDPKTSR-UKTHLTGXSA-N
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2015
• 出版时间：15 November 2015
• 年：2015
• 卷：25
• 期：22
• 页码：5028-5031
• 全文大小：456 K

文摘

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.