Amides of non-steroidal anti-inflammatory drugs with thiomorpholine can yield hypolipidemic agents with improved anti-inflammatory activity

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• 作者：Panagiotis Theodosis-Nobelos ; Malamati Kourti ; Antonios Gavalas ; Eleni A. Rekka ; ^{rekka@pharm.auth.gr" class="auth_mail" title="E-mail the corresponding author}
• 关键词：YOTNQUFXENRSSG-UHFFFAOYSA-N ; YMZGMGYHDFIFKV-UHFFFAOYSA-N ; NRSSJYANCHFWBR-UHFFFAOYSA-N ; BNZZWLFDWYKVRS-UHFFFAOYSA-N ; SEAXJFIBZAIKMX-UHFFFAOYSA-N ; ULEYWVJMDABIKF-UHFFFAOYSA-N ; BKAYNJMLPCTTHC-UHFFFAOYSA-N ; NGELFMBYIVBTIS-UHFFFAOYSA-N ; ADCSEMOQPOEWPY-UHFFFAOYSA-N ; DRMIZEBSAJBMSW-UHFFFAOYSA-N
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2016
• 出版时间：1 February 2016
• 年：2016
• 卷：26
• 期：3
• 页码：910-913
• 全文大小：330 K

文摘

Novel amides of non steroidal anti-inflammatory drugs (NSAIDs), α-lipoic acid and indole-3-acetic acid with thiomorpholine were synthesised by a simple method and at high yields (60–92%). All the NSAID derivatives highly decreased lipidemic indices in the plasma of Triton treated hyperlipidemic rats. The most potent compound was the indomethacin derivative, which decreased total cholesterol, triglycerides and LDL cholesterol by 73%, 80% and 83%, respectively. They reduced acute inflammation equally or more than most parent acids. Hence, it could be concluded that amides of common NSAIDs with thiomorpholine acquire considerable hypolipidemic potency, while they preserve or augment their anti-inflammatory activity, thus addressing significant risk factors for atherogenesis.