Abstract
A series of 15 chalcones-bearing substituents at positions 2, 4, and 5 of rings A and B were synthesized using microwave-assisted Claissen–Smichdt condensation and evaluated for their activity against Giardia lamblia and Green monkey kidney cells. Five compounds exhibited activity against G. lamblia at IC50’s <5 μM. The chalcone 3m exhibited the highest antigiardial activity (IC50 = 1.03 μM), even more than the positive control (metronidazole, IC50 = 1.4 μM), and selectivity (SI = 38.9). A preliminary SAR study suggested that electrophylicity has not relationship with antigiardiasic activity, and the docking study reveals that synthesized chalcones bind at zone 3 of colchicine site, therefore presumably the action mechanism of the synthesized chalcones does not follow the Michael acceptor mechanism.
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