Abstract
3-[(2-Chloroquinolin-3-yl) methylene]-5-phenylfuran-2(3H)-one derivatives (6a–j and 7a–j) have been synthesized and evaluated for their antimalarial activity. Three compounds 7d, 7f, and 7g showed excellent activity (0.50–0.72 µg/mL). In addition, six compounds were active in range below 5 µg/mL. A preliminary structure–activity relationship analysis of the series suggested that electropositive character is beneficial for antimalarial activity. Falcipain-2 was identified as potential target for the compounds by in silico studies. The docking studies of synthesized compounds on falcipain-2 revealed vital interactions and their binding conformation. Compound 7d and 7f could be used as lead to develop selective falcipain-2 inhibitors as they showed good inhibition of the enzyme in enzyme assay studies.
Published Version
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