Synthesis of chalcone derivatives by Claisen-Schmidt condensation and in vitro analyses of their antiprotozoal activities
| Autor: | Gabriella B. Souza, Tamiris A. C. Santos, Amanda P. S. Silva, André L. B. S Barreiros, Victória Brandão Nardelli, Ingrid B. Siqueira, Silvio S. Dolabella, Emmanoel.V. Costa, Péricles B. Alves, Ricardo Scher, Roberta P. M. Fernandes |
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| Rok vydání: | 2022 |
| Předmět: | |
| Zdroj: | Natural Product Research. :1-8 |
| ISSN: | 1478-6427 1478-6419 |
| DOI: | 10.1080/14786419.2022.2140337 |
| Popis: | Chalcone is a molecule with known biological activities. Based on this, a series of chalcone derivatives bearing methyl, phenyl or furanyl substituents at different positions of A and B rings were synthesised, characterised, and evaluated regarding antiprotozoal activity. Molecules were synthesised via base catalyzed Claisen-Schmidt condensation and characterised by IR and NMR spectral data. Antiprotozoal activity against Phytomonas serpens, Leishmania amazonensis and Acanthamoeba polyphaga was performed. All compounds inhibited more than 50% of the growth of P. serpens while five had this effect on L. amazonensis and all of them no more than 35% of inhibition on A. polyphaga. Remarkably interesting antiprotozoal effects were recorded with compound 5, with IC50 of 1.59 µM for P. serpens and 11.49 µM for L. amazonensis. The addition of a naphthyl group to the B ring can be postulated to be the cause of the 10 times increase observed in its trypanocidal activity. |
| Databáze: | OpenAIRE |
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