In Vivo Antimalarial Evaluation Of Embelin And Some Semi- Synthetic Aromatic Amine Substituted Embelin Derivatives From The Fruit Of Embelia Schimperia

Malaria is a major public health problem mainly due to the development of drug resistancernby the most lethal causative parasitic species. New drugs with unique structures andrnmechanism of action are urgently required to treat sensitive and drug-resistant strains ofrnmalaria. Historically, compounds containing novel structure from natural origin represent arnmajor source for the discovery and development of new drugs for several diseases. Thernpresent study aimed at isolating embelin from the fruit of Embelia schimperia, preparingrnsome semi-synthesized compounds starting from embelin and evaluating of their in vivornantimalarial activities against mice infected with Plasmodium berghei using a 4-daysrnsuppressive test.rnThree novel aromatic substituted embelin derivatives were semi-rnsynthesized in good yields (>98%) by using one-step condensation reaction. Structures forrnthe synthesized compounds were determined using IR, 1H NMRrn13rnC NMR and MS. Anrnattempt has been made in this study to provide some insight on recent semisyntheticrnapproaches to antimalarial drug discovery from natural sources with some structuralrnmodification.rnThe target compounds, at a dose of 100-400 mg/kg, suppressed P. berghei parasites by 49-rn75% which was significantly different from the negative control group (P

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