Abstract

Over the last decade, there has been an increasing effort to fight inflammatory conditions establishing new multitarget approaches. Chronic inflammation is implicated in many multifactorial diseases, constituting a great economic burden and a chronic health problem. In an attempt to develop new potent multifunctional anti-inflammatory agents, a cinnamic-pyrrole hybrid (6) was synthesized and screened for its antioxidant and anti-Lipoxygenase potential. The new compound, in comparison with its pyrrole precursor (4), showed improved biological activities. In silico calculations were performed to predict its drug-likeness. The examined derivative is considered orally bioavailable according to Lipinski’s rule of five. Compound 6 could be used as a lead for the synthesis of more effective hybrids.

Highlights

  • IntroductionOverproduction of free radicals and depletion of the cellular antioxidant capacity can have detrimental effects on biomacromolecules, by means of lipid peroxidacapacity can have detrimental effectsmutation on biomacromolecules, by means of lipid peroxition, protein impairment and DNA and damage [20]

  • These agents had an increased risk of cardiovascular side effects owing to reduction in endothelial prostaglandin I2 (PGI2 ) and increased levels of platelet aggregator thromboxane A2 (TXA2 ) [4,5]

  • In light of the above, we report theinsynthesis a new pyrrole-cinnamic acid (4)

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Summary

Introduction

Overproduction of free radicals and depletion of the cellular antioxidant capacity can have detrimental effects on biomacromolecules, by means of lipid peroxidacapacity can have detrimental effectsmutation on biomacromolecules, by means of lipid peroxition, protein impairment and DNA and damage [20]. It is imperative dation, protein impairment and mutation of and damage [20]. It is imperative that research should focus on theDNA development new multifunctional agents combining that researchand should focus on the development antioxidant anti-inflammatory activities. Of new multifunctional agents combining antioxidant anti-inflammatory.

Results and Discussion
Physicochemical Studies
Biological Evaluation
General Information
Chemistry General Procedure
Biological In Vitro Assays
Inhibition of Linoleic Acid Lipid Peroxidation
Inhibition of Soybean Lipoxygenase In Vitro
Conclusions
Full Text
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