Abstract
The aim of the study was to optimize the synthesis of diclofenac derivative with hydrazones structure in order to obtain higher yields and purity by variation of different parameters such as: ratio between reactants, solvent, catalyst, temperature, time of reaction and method used. The anti-inflammatory effects of diclofenac derivatives were evaluated using in vitro assays: albumin denaturation and erythrocyte membrane stability. The obtained results showed that the effect of the tested derivatives is increasing with the concentration, the best results being obtained at the concentration of 125 �g/mL (albumin denaturation assay), respectively 111.11 �g/mL (erythrocyte membrane stability assay). The most active compound was 4d which showed the highest inhibition effect on albumin denaturation and an appreciable effect on erythrocyte membrane stability, in comparation with diclofenac, used as drug reference.
Highlights
Non-steroidal anti-inflammatory drugs (NSAIDs) are among the oldest and most successful drugs known in modern medicine to decrease pain and inflammation by inhibiting prostaglandins synthesis, but their use is associated with a number of serious side effects
In order to improve the pharmacological profile of diclofenac, some hydrazone derivatives were synthesized by researchers [5,6]
The aim of this study was to optimize the method for synthesis of diclofenac derivatives with hydrazone structure in order to apply it for extending the diclofenac hydrazone derivatives library
Summary
Non-steroidal anti-inflammatory drugs (NSAIDs) are among the oldest and most successful drugs known in modern medicine to decrease pain and inflammation by inhibiting prostaglandins synthesis, but their use is associated with a number of serious side effects. NSAIDs, such as diclofenac, are indicated for improvement of all degrees inflammation associated with a large number of conditions, including arthritic disorders, acute musculoskeletal disorders and other painful conditions resulted from trauma. If gastrointestinal bleeding or ulceration occurs to patients who receive diclofenac, treatment will be ended [1,2]. Hydrazone derivatives represent an attractive group of compounds with a broad spectrum of pharmacological and biological characteristics [3,4]. In order to improve the pharmacological profile of diclofenac, some hydrazone derivatives were synthesized by researchers [5,6]
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