| Full text | |
| Author(s): |
da Rocha Pissurno, Ana Paula
[1]
;
Santos, Fernanda Amorim
[1]
;
Bolela Bovo Candido, Ana Carolina
[2]
;
Magalhaes, Lizandra Guidi
[2]
;
de Laurentiz, Rosangela da Silva
[1]
Total Authors: 5
|
| Affiliation: | [1] Univ Estadual Paulista, Fac Engn Ilha Solteira, Dept Fis & Quim, Sao Paulo - Brazil
[2] Univ Franca, Nucleo Pesquisas Ciencias Exatas & Tecnol, Franca, SP - Brazil
Total Affiliations: 2
|
| Document type: | Journal article |
| Source: | MEDICINAL CHEMISTRY RESEARCH; v. 27, n. 9, p. 2224-2229, SEP 2018. |
| Web of Science Citations: | 0 |
| Abstract | |
A series of lactone 1,4-dihydroquinoline derivatives 4 (4 and 4aa-4cm) was screened for in vitro antileishmanial activity against the promastigote form of Leishmania (Leishmania) amazonensis. Screening results indicate that all of the synthesized compounds significantly reduced the growth of promastigote forms of promastigotes of L. (L.) amazonensis. The cytotoxicity of the most active compounds was also measured on peritoneal macrophage cells. Compounds 4ah and 4bn showed better activities than other derivatives with IC50 values of 6.22 and 9.05 mu M, respectively, with selectivity index 22 and 15 times less toxicity to macrophages cells than to parasites, respectively. The experimental data propose that the compounds may be further investigated against amastigote forms and may contribute to the search of new candidates drugs for treatment of cutaneous leishmaniasis. (AU) | |
| FAPESP's process: | 14/07493-5 - Synthesis and biological evaluation of heterocyclic compounds, analogs of lignans, obtained by microwave-assisted multi-component reactions |
| Grantee: | Rosangela da Silva de Laurentiz |
| Support Opportunities: | Regular Research Grants |
| FAPESP's process: | 16/24456-1 - Monoketo enone curcuminoids the treatment of schistosomiasis: an pre-clinical evaluation of schistosomicidal activity |
| Grantee: | Lizandra Guidi Magalhães |
| Support Opportunities: | Regular Research Grants |
| FAPESP's process: | 15/01394-8 - Study of EF-24 curcumin analogue and praziquantel in biochemical and morphological aspects involved in the cell death of the Schistosoma mansoni parasite |
| Grantee: | Fernanda Rafacho Badoco |
| Support Opportunities: | Scholarships in Brazil - Master |