Facile synthesis and in-vitro antimalarial activity of novel α-hydroxy hydrazonates

A series of previously unreported α-hydroxy hydrazonates were synthesized and tested for their antimalarial properties. Structure optimization of the antiplasmodially active α-hydroxy hydrazonate III furnished derivatives with strong in-vitro antimalarial activity against 3D7 strains of Plasmodium falciparum with IC ₅₀ values lower than 2.0 μM. Novel α-hydroxy hydrazonates were prepared and evaluated as antiplasmodials. Remarkable antiplasmodial activity was ascertained for compounds 4r, 5d and 4q with IC ₅₀ values of 0.6, 0.85 and 1.1 μM, making these α-hydroxy hydrazonates promising candidates for further drug design.