Pharmacokinetic evaluation of Chalcone derivatives with antimalarial activity in New Zealand White Rabbits

Abstract Objective Malaria is a major global health concern with the urgent need for new treatment alternatives due to alarming increase of drug-resistant Plasmodium strains. Chalcones and its derivatives are important pharmacophores showing antimalarial activity. Determination pharmacokinetic variables at preliminary step drug development any candidates an essential component in vivo efficacy tests. Substandard often responsible insufficient therapeutic effect. Therefore, three chalcone derivatives, 1, 2, 3, having potency were studied further potential efficacy. Results In studies these performed on New Zealand White rabbits. The administered intra-peritoneally or orally effective dose concentration blood samples different time points collected. determination was done through reverse phase-high performance liquid chromatography. peak plasma derivative 3 1.96 ± 0.46 µg/mL (intraperitoneal route), 69.89 5.49 (oral 3.74 1.64 route). results indicate very low bioavailability derivatives. present study gives benchmark advance investigation more order revamp while maintaining both metabolic constancy.