Synthesis and Antimalarial Properties of Three Substituted Trinitro-Tribenzylamine

Abstract

Malaria infection is a major health burdens in Tropical Africa and this is made worst with the emergence of Plasmodium falciparum resistance to the commonly used antimalarial drugs. There is therefore the need for new potent antimalarial drugs. Syntheses of o-trinitro tribenzylamine (2TBN), m-trinitro tribenzylamine (3TBN) and p-trinitro tribenzylamine (4TBN) were carried and yields of 38.49%, 41.01% and 39.67% respectively were obtained on reacting the respective o-, m-, and p-nitro benzaldehyde with formamide. The three synthesized trinitro-tribenzylamine derivatives were tested in vitro against Plasmodium falciparum isolates (3D7 strain) using parasite lactate dehydrogenase assay (pLDH). The result showed significant activity with IC₅₀ ranging from 18 to 30 nM. The meta derivative (IC₅₀:18.823 nM) showed better antiplasmodial activity than ortho (IC₅₀: 30.287 nM) and para (IC₅₀: 22.297 nM) derivatives, and even chloroquine phosphate (IC₅₀: 22.777 nM).