What is it about?

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. 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.

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Why is it important?

The 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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This page is a summary of: Synthesis, in vitro antigiardial activity, SAR analysis and docking study of substituted chalcones, Medicinal Chemistry Research, December 2019, Springer Science + Business Media,
DOI: 10.1007/s00044-019-02492-5.
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