A series of 3-substituted-2-hydroxy-1,4-naphthoquinone derivatives with a variety side chains were successfully synthesized by Mannich reaction 2-hydroxy-1,4-naphthoquinone (lawsone) selected amines and aldehydes. All substances (1–16) evaluated for in-vitro antimalarial activity against strains Plasmodium falciparum microculture radioisotope technique. Bioassay data revealed that ten (1–8, 11 ...

Malaria remains the worlds’ most devastating human parasitic infection, afflicting 500 million people and causing from 1.7-2.5 million deaths each year globally. 4-aminoquinoline drugs are highly effective and rapidly acting agents against asexual erythrocytic stages of malaria parasites mainly P. vivax and P. falciparum responsible for life threatening clinical manifestations and severity of t...

The high antiplasmodial activity of racemic benzylamines rac-1 and rac-2 stimulated the synthesis of pure enantiomers. Ellman's chiral sulfinamides (S)-6 and (R)-6 were used as chiral auxiliaries. Condensation of prochiral ketone 5 with enantiomerically pure sulfinamides (S)-6 and (R)-6 and subsequent NaBH4 reduction provided predominantly unlike configured diastereomers (S,R)-8 and (R,S)-8 (ra...

This paper describes the synthesis and in vitro antimalarial activity against a P. falciparum 3D7 strain of some new 1-aryl-3-substituted propanol derivatives. Twelve of the tested compounds showed an IC(50) lower than 1 microM. These compounds were also tested for cytotoxicity in murine J774 macrophages. The most active compounds were evaluated for in vivo activity against P. berghei in a 4-da...

Abstract: A new series of plasmepsin II (PM II) inhibitors has been prepared based on 4-aminopiperidine-tert-butyl-carbamate (1). These compounds might be useful as antimalarial drugs acting via a new mechanism, and therefore be less susceptible to parasite resistance now often observed with current antimalarial therapies. Some of the final compounds prepared exhibited encouraging inhibitory ac...

Infections caused by protozoan parasites continue to be a significant cause of morbidity and mortality across the globe, with malaria leishmaniasis forming fulcrum these infections. Decreased effectiveness existing drugs increasing cases drug resistance have called for multifaceted approach development safe, efficacious, affordable leishmaniasis. The present review article aims unearth structur...