BIOPHARMACEUTICAL CHARACTERISTICS AND IN VITRO EVALUATION OF THE REDUCING ANTIOXIDANT POWER OF SOME DICLOFENAC DERIVATIVES
Abstract
Aim: Biopharmaceutical characterization using the prediction program MedChemDesigner 5.5 and the evaluation of the reducing antioxidant power of some diclofenac derivatives. Material and methods: The synthesized compounds (4a-s) were characterized in silico, by estimation of octanol/water partition coefficient (OWPC), octanol/water distribution coefficient (OWDC), absorptive capacity at digestive level, and topological polar surface area. The evaluation of antioxidant power was performed using in vitro methods: ferric and phosphomolybdenum reducing antioxidant power assays. Results: The biopharmaceutical characteristics suggest an optimal pharmacokinetic profile with a lipophilic character of the studied derivatives, which allows both the crossing of cell membranes and digestive tract absorption. In addition, several compounds have demonstrated notable antioxidant capacity, higher than that of diclofenac. The most active compounds were 4s (R=2-Br-3-OH-4-OCH3) and 4h (R=H). Conclusions: The biopharmaceutical study revealed promising characteristics regarding the pharmacokinetic profile of the studied compounds. Moreover, it was noticed that the antioxidant effect increases with concentration and is influenced by the nature of the substituent in the aromatic ring.
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