SYNTHESIS AND ANTIPLASMODIAL ACTIVITY OF SOME NOVEL CHALCONE DERIVATIVES
Journal Title: Asian Journal of Pharamceutical and Clinical Research - Year 2015, Vol 8, Issue 2
Abstract
Increased drug resistance in malaria toward many of the existing antimalarials make the condition worse. Hence, indicates the necessity of thenovel molecules to overcome the problem. A series of chalcone derivatives (3a-4e) were primed via Claisen-Schmidt condensation of substitutedaldehydes with substituted methyl ketones. These derivatives were tested against Plasmodium falciparum clinical isolate for their antiplasmodialactivity. Furthermore, in-vitro β-hematin formation assay has been conducted in order to gain insight into the possible mechanism of action. Outof the 10 synthesized compounds, two compounds 4a and 4d exhibited promising antiplasmodial activities (50% inhibitory concentration [IC50]values 7.45±0.65 and 6.01±0.29 μg/ml, respectively). Other compounds (3a, 4b, 4e and 3d) showed moderate inhibition against P. falciparum. Amongall the compounds, 4a showed good hemozoin inhibitory activity (IC50 - 19.75 μg/ml) while 3a and 4d showed moderate type inhibition. Thesemolecules may act as templates for medicinal chemistry to discover novel and hybrid molecules with improved characteristics, which may becomefuture candidates for the treatment of malaria.Keywords: Chalcone, Malaria, Plasmodium falciparum, β-hematin.Â
Authors and Affiliations
Neetu Tomar, Shiv Vardan Singh, Chottes Lal Jain, Gaurav Verma, Anirban Pal, Vineeta Singh
Keywords
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