Malaria stills on the top of the devastating diseases in the world. On yearly basis, approximately 600,000 million people are infected and a million dies because of this disease. One of the major problems is that parasites have become resistant to drugs currently available. Consequently, there is a need to find new anti-malarial agents. Chalcones and their derivatives are some of the many occurring natural products that exhibit a broad range of biological activities, including antimalarial potential. It is known that replacing one of the aromatic rings of a chalcone with a ferrocenyl group results in a potential enhancement, presumably due to the lipophilicity of the ferrocenyl group and bioavailability. Moreover, according to the literature, the presence of aromatic heterocyclic moieties in the molecule’s scaffold improves their potential as antimalarial active compounds. Therefore, it is expected that ferrocenyl chalcones based scaffolds containing heterocyclic moieties will exhibit antimalarial activity. Ferrocenyl chalcones with a variety of heterocyclic moieties were synthesized by a solvent free base catalyzed Claisen-Schmidt reaction. Pure products of moderate to good yields have been obtained and purity has been confirmed via <sup>1</sup>H-NMR and <sup>13</sup>C-NMR spectroscopy as well as melting points determinations. Synthetic methodology, characterization, and preliminary bioassays in malaria of these compounds will be elaborated. This research is supported by MARC grant 2T34GM007821-36.

Ferrocenyl chalcones based scaffolds containing heterocyclic moieties as potential antimalarial agents

251st National Meeting (2016)

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