Active Anti-Inflammatory and Hypolipidemic Derivatives of Lorazepam.

Abstract

Novel derivatives of some non steroidal anti-inflammatory drugs, as well as of the antioxidants α-lipoic acid, trolox and (E)-3-(3,5-di-tert-butyl-4-hydroxyphenyl)acrylic acid with lorazepam were synthesised by a straightforward method at satisfactory to high yields (40%-93%). All the tested derivatives strongly decreased lipidemic indices in rat plasma after Triton induced hyperlipidaemia. They also reduced acute inflammation and a number of them demonstrated lipoxygenase inhibitory activity. Those compounds acquiring antioxidant moiety were inhibitors of lipid peroxidation and radical scavengers. Therefore, the synthesised compounds may add to the current knowledge about multifunctional agents acting against various disorders implicating inflammation, dyslipidaemia and oxidative stress.

• Authors: Panagiotis Theodosis-Nobelos, Georgios Papagiouvannis, Panos N Kourounakis, Eleni A Rekka
• Journal: Molecules (Basel, Switzerland) (Molecules) Vol. 24 Issue 18 (Sep 09 2019) ISSN: 1420-3049 [Electronic] Switzerland
• PMID: 31505754 (Publication Type: Journal Article)

Chemical References

• Acrylates
• Anti-Inflammatory Agents, Non-Steroidal
• Antioxidants
• Chromans
• Hypolipidemic Agents
• Lipoxygenase Inhibitors
• Thioctic Acid
• Carrageenan
• acrylic acid
• Lorazepam
• 6-hydroxy-2,5,7,8-tetramethylchroman-2-carboxylic acid

Topics

• Acrylates (pharmacology)
• Animals
• Anti-Inflammatory Agents, Non-Steroidal (chemistry, pharmacology)
• Antioxidants (chemistry, pharmacology)
• Carrageenan (chemistry, pharmacology)
• Chromans (chemistry, pharmacology)
• Humans
• Hyperlipidemias (drug therapy, pathology)
• Hypolipidemic Agents (chemistry, pharmacology)
• Inflammation (drug therapy)
• Lipid Peroxidation (drug effects)
• Lipoxygenase Inhibitors (pharmacology)
• Lorazepam (analogs & derivatives, pharmacology)
• Oxidative Stress (drug effects)
• Rats
• Thioctic Acid (analogs & derivatives, pharmacology)