Bioorganic and Medicinal Chemistry Letters p. 3034 - 3036 (2011)
Update date:2022-08-03
Topics: Medicinal chemistry Resistance Structure-Activity Relationship (SAR) Pharmacokinetics Toxicity and Safety Target Identification Efficacy Testing
Aher, Rahul Balasaheb
Wanare, Gajanan
Kawathekar, Neha
Kumar, Ravi Ranjan
Kaushik, Naveen Kumar
Sahal, Dinkar
Chauhan, Virander Singh
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 IC50 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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