Antiprotozoal quinolines containing electrophilic moieties

Abstract

Compounds containing the quinoline moiety have been the mainstay of antimalarial chemotherapy. However, the emergence of resistant strains of Plasmodium falciparum, the causative agent of malaria, has compromised the efficacy of these antimalarial quinolines. Therefore the development of new efficient drugs is of critical importance. Extensive research has identified the cysteine proteases in malaria and other parasitic diseases as potential targets for new chemotherapy due to their critical roles in the life cycles of the causative agents. Due to their role in the antimalarial activity of clinically available drugs, quinolines were used as scaffolds to which electrophilic groups, such as thiosemicarbazone, a,β-unsaturated ketone and pyrazoline moieties were appended.