Malaria has been a major cause of morbidity and mortality in developing countries, particularly in Sub-Saharan
Africa and South Asia. The global malaria situation is increasingly being challenging owing to lack of credible malaria
vaccine and the emergence of drug resistance to most of the available antimalarials. They demand search for novel
generation of drugs. Versatility and flexibility for structural modification of natural and synthetic analogues of curcumin
and chalcone have been explored extensively for designing new antimalarial agent. Recent advances to our knowledge of
parasite biology as well as the availability of the genome sequence, have opened up new vista in the firmament of
antimalarial drug designing for identifying novel molecular targets. Curcumin and chalcones has been reported to exert
anti-malarial effect by binding directly to numerous signaling molecules, such as histone acetyltransferase, histone
deacetylase, sarco (endo) plasmic reticulum Ca2+-ATPase, cysteine proteases etc. This review highlights insights the more
recent antimalarial activities of these compounds, their mechanisms of action, molecular targets and relevant structureactivity
relationship studies. Natural lead compounds like chalcone and curcumin have shown good and optimal binding
to many enzymes present in parasite and can be explored as molecular targets for in silico studies to develop new,
affordable and effective antimalarial drugs. With no credible malaria vaccine in sight, there is an imperative need to
develop new drugs with different mechanisms of action to help preclude issues of cross-resistance.
Keywords: Antimalarial, Bioavailability, Chalcone, Curcumin, Molecular Targets, Histone acetyltransferase.
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