Literature DB >> 26750253

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

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.
Copyright © 2015 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Hypolipidemic activity; Inflammation; Non steroidal anti-inflammatory drugs; Thiomorpholine amides; α-Lipoic acid

Mesh:

Substances:

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


  6 in total

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2.  Ionic Liquid-assisted Synthesis of Celexocib Using Tris-(2-hydroxyethyl) Ammonium Acetate as an Efficient and Reusable Catalyst.

Authors:  Hamid Reza Ahfad-Hosseini; Hasan Bagheri; Salimeh Amidi
Journal:  Iran J Pharm Res       Date:  2017       Impact factor: 1.696

3.  Enantioselective Hydrocarbamoylation of Alkenes.

Authors:  Sheng Feng; Yuyang Dong; Stephen L Buchwald
Journal:  Angew Chem Int Ed Engl       Date:  2022-06-23       Impact factor: 16.823

4.  A Bio-Guided Screening for Antioxidant, Anti-Inflammatory and Hypolipidemic Potential Supported by Non-Targeted Metabolomic Analysis of Crepis spp.

Authors:  Christina Barda; Konstantina Anastasiou; Ariadni Tzara; Maria-Eleni Grafakou; Eleftherios Kalpoutzakis; Joerg Heilmann; Michael Rallis; Angeliki P Kourounakis; Helen Skaltsa
Journal:  Molecules       Date:  2022-09-20       Impact factor: 4.927

5.  Active Anti-Inflammatory and Hypolipidemic Derivatives of Lorazepam.

Authors:  Panagiotis Theodosis-Nobelos; Georgios Papagiouvannis; Panos N Kourounakis; Eleni A Rekka
Journal:  Molecules       Date:  2019-09-09       Impact factor: 4.411

6.  Design, Synthesis and Study of Nitrogen Monoxide Donors as Potent Hypolipidaemic and Anti-Inflammatory Agents.

Authors:  Panagiotis Theodosis-Nobelos; Georgios Papagiouvanis; Maria Pantelidou; Panos N Kourounakis; Chrysoula Athanasekou; Eleni A Rekka
Journal:  Molecules       Date:  2019-12-19       Impact factor: 4.411

  6 in total

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