Synthesis, in vitro antigiardial activity, SAR analysis and docking study of substituted chalcones

  • David Cáceres-Castillo, Rubén M. Carballo, Ramiro Quijano-Quiñones, Gumersindo Mirón-López, Manlio Graniel-Sabido, Rosa E. Moo-Puc, Gonzalo J. Mena-Rejón
  • Medicinal Chemistry Research, December 2019, Springer Science + Business Media
  • DOI: 10.1007/s00044-019-02492-5

A series of 15 chalcones were evaluated for their activity against Giardia lamblia

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.

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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http://dx.doi.org/10.1007/s00044-019-02492-5

The following have contributed to this page: Dr Gonzalo J. Mena-Rejón