4.4 Article

Synthesis of chalcone derivatives by Claisen-Schmidt condensation and in vitro analyses of their antiprotozoal activities

Journal

NATURAL PRODUCT RESEARCH
Volume -, Issue -, Pages -

Publisher

TAYLOR & FRANCIS LTD
DOI: 10.1080/14786419.2022.2140337

Keywords

Phytomonas serpens; Leishmania amazonensis; Acanthamoeba polyphaga; Chalcone

Funding

  1. Brazil Conselho Nacional de Desenvolvimento Cientifico e Tecnologico (CNPq)
  2. Brazil Fundacao de Apoio a Pesquisa e a Inovacao Tecnologica do Estado de Sergipe (Fapitec/SE)
  3. Brazil Coordenacao de Aperfeicoamento de Pessoal de Nivel Superior (CAPES) [001]
  4. Brazil Financiadora de Estudos e Projetos (FINEP)

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A series of chalcone derivatives with different substituents were synthesized and evaluated for their antiprotozoal activity. One compound showed remarkable inhibitory effects on the growth of certain protozoa.
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 mu M for P. serpens and 11.49 mu M 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.

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