Examining barbiturate scaffold for the synthesis of new agents with biological interest

Barbiturates have a long history of being used as drugs presenting wide varieties of biological activities (antimicrobial, anti-urease and antioxidant). Reactive oxygen species are associated with inflammation implicated in cancer, atherosclerosis and autoimmune diseases. Multitarget agents represen...

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Bibliographic Details
Published in:Future medicinal chemistry 2019-08, Vol.11 (16), p.2063-2079
Main Authors: Katsamakas, Sotirios, Papadopoulos, Anastasios G, Kouskoura, Maria G, Markopoulou, Catherine K, Hadjipavlou-Litina, Dimitra
Format: Article
Language:English
Subjects:
Amino acids
anti-inflammatory agents
Antioxidants
Arteriosclerosis
Autoimmune diseases
autotaxin inhibitors
Barbiturates
cyclooxygenase inhibitors
Cyclooxygenase-2
DFT study
Drugs
Energy
Enzymes
hybrid barbiturates
Inflammation
Inflammatory diseases
Ligands
lipoxygenase inhibitors
molecular modeling
multitarget compounds
phosphodiesterase inhibitors
pleiotropic agents
Proteins
Reactive oxygen species
Software
Solvents
Urease
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Summary:Barbiturates have a long history of being used as drugs presenting wide varieties of biological activities (antimicrobial, anti-urease and antioxidant). Reactive oxygen species are associated with inflammation implicated in cancer, atherosclerosis and autoimmune diseases. Multitarget agents represent a powerful approach to the therapy of complicated inflammatory diseases. A novel series of barbiturates has been synthesized and evaluated in several assays. Compound (lipoxygenases inhibitor, 55.0 μM) was found to be a cyclooxygenase-2 inhibitor (27.5 μM). Compound was profiled as a drug-like candidate. The barbiturate core represents a new scaffold for lipoxygenases inhibition, and the undertaken derivatives show promise as multiple-target agents to combat inflammatory diseases.
ISSN:1756-8919
1756-8927
DOI:10.4155/fmc-2018-0541