BIOPHARMACEUTICAL CHARACTERISTICS AND IN VITRO EVALUATION OF THE REDUCING ANTIOXIDANT POWER OF SOME DICLOFENAC DERIVATIVES

  • A. FOCȘA “Grigore T. Popa” University of Medicine and Pharmacy Iasi
  • Ioana VASINCU “Grigore T. Popa” University of Medicine and Pharmacy Iasi
  • A. SAVA “Grigore T. Popa” University of Medicine and Pharmacy Iasi
  • Andreea IACOB “Grigore T. Popa” University of Medicine and Pharmacy Iasi
  • Maria APOTROSOAEI “Grigore T. Popa” University of Medicine and Pharmacy Iasi
  • Lenuța PROFIRE “Grigore T. Popa” University of Medicine and Pharmacy Iasi

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.

Author Biographies

A. FOCȘA, “Grigore T. Popa” University of Medicine and Pharmacy Iasi

Faculty of Pharmacy
Department of Pharmaceutical Chemistry

Ioana VASINCU, “Grigore T. Popa” University of Medicine and Pharmacy Iasi

Faculty of Pharmacy
Department of Pharmaceutical Chemistry

A. SAVA, “Grigore T. Popa” University of Medicine and Pharmacy Iasi

Faculty of Pharmacy
Department of Pharmaceutical Chemistry

Andreea IACOB, “Grigore T. Popa” University of Medicine and Pharmacy Iasi

Faculty of Pharmacy
Department of Pharmaceutical Chemistry

Maria APOTROSOAEI, “Grigore T. Popa” University of Medicine and Pharmacy Iasi

Faculty of Pharmacy
Department of Pharmaceutical Chemistry

Lenuța PROFIRE, “Grigore T. Popa” University of Medicine and Pharmacy Iasi

Faculty of Pharmacy
Department of Pharmaceutical Chemistry

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Published
2020-09-30