| Literature DB >> 26750253 |
Panagiotis Theodosis-Nobelos1, Malamati Kourti1, Antonios Gavalas1, Eleni A Rekka2.
Abstract
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.Entities:
Keywords: Hypolipidemic activity; Inflammation; Non steroidal anti-inflammatory drugs; Thiomorpholine amides; α-Lipoic acid
Mesh:
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Year: 2015 PMID: 26750253 DOI: 10.1016/j.bmcl.2015.12.063
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN: 0960-894X Impact factor: 2.823