| Texto completo | |
| Autor(es): |
Silva, Matheus L.
;
Baldim, Joao L.
;
Costa-Silva, Thais A.
;
Amaral, Maiara
;
Romanelli, Maiara M.
;
Levatti, Erica V. C.
;
Tempone, Andre G.
;
Lago, Joao Henrique G.
Número total de Autores: 8
|
| Tipo de documento: | Artigo Científico |
| Fonte: | Journal of the Brazilian Chemical Society; v. 36, n. 8, p. 7-pg., 2025-01-01. |
| Resumo | |
In the present work, three series of cinnamic (1), p-coumaric (2) and ferulic (3) esters containing different side-chains such as ethyl (1a-3a), n-propyl (1b-3b), n-butyl (1c-3c), n-pentyl (1d-3d), n-hexyl (1e-3e), and n-heptyl (1f-3f) were prepared, tested for activity against trypomastigote forms of the parasite Trypanosoma cruzi and toxicity against NCTC cells. Obtained results indicated that the presence of p-coumaric or ferulic moieties associated with C4-C7 linear side-chains play an important role in the bioactivity against T. cruzi since compounds 2c-2f and 3d-3f were found to be the most active derivatives with a half maximal effective concentration (EC50) value ranging from 12.8 to 1.7 mu M, superior to that determined for the positive control benznidazole (EC50 = 16.4 mu M). Additionally, machine learning and multivariate statistical analyses identified molecular features correlated with biological activity, emphasizing the importance of side-chain length and lipophilicity, highlighting the significance of the molecular structure of phenylpropanoid derivatives in the activity against T. cruzi. (AU) | |
| Processo FAPESP: | 23/12447-1 - Busca de metabólitos especializados oriundos da biodiversidade florística brasileira como candidatos a fármacos para doenças tropicais negligenciadas |
| Beneficiário: | João Henrique Ghilardi Lago |
| Modalidade de apoio: | Auxílio à Pesquisa - Programa BIOTA - Regular |