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Published on: July 11, 2025
Dibenzylideneacetone analogues as novel Plasmodium falciparum inhibitors
Rahul Balasaheb Aher1, Gajanan Wanare, Neha Kawathekar
1Department of Pharmacy, Shri G.S. Institute of Technology and Science, 23 Park Road, Indore 452003 (MP), India. rahulba26@yahoo.co.in
Abstract:
A series of dibenzylideneacetones (A1-A12) and some of their pyrazolines (B1-B4) were synthesized and evaluated in vitro for blood stage antiplasmodial properties in Plasmodium falciparum culture using SYBR-green-I fluorescence assay. The compound (1E, 4E)-1,5-bis(3,4-dimethoxyphenyl)penta-1,4-dien-3-one (A9) was found to be the most active with IC(50) of 1.97 μM against chloroquine-sensitive strain (3D7) and 1.69 μM against chloroquine-resistant field isolate (RKL9). The MTT based cytotoxicity assay on HeLa cell line has confirmed that A9 is selective in its action against malaria parasite (with a therapeutic index of 166). Our results revealed that these compounds exhibited promising antiplasmodial activities which can be further explored as potential leads for the development of cheaper, safe, effective and potent drugs against chloroquine-resistant malarial parasites.
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