| Full text | |
| Author(s): Show less - |
Luczywo, Ayelen
;
Gonzalez, Lucia G.
;
Aguiar, Anna C. C.
;
Oliveira de Souza, Juliana
;
Souza, Guilherme E.
;
Oliva, Glaucius
;
Aguilar, Luis F.
;
Casal, Juan J.
;
Guido, Rafael V. C.
;
Asis, Silvia E.
;
Mellado, Marco
Total Authors: 11
|
| Document type: | Journal article |
| Source: | NATURAL PRODUCT RESEARCH; v. 36, n. 15, p. 7-pg., 2021-02-24. |
| Abstract | |
Malaria is an infectious illness, affecting vulnerable populations in Third World countries. Inspired by natural products, indole alkaloids have been used as a nucleus to design new antimalarial drugs. So, eighteen oxindole derivatives, aza analogues were obtained with moderate to excellent yields. Also, the saturated derivatives of oxindole and aza derivatives via H-2/Pd/C reduction were obtained in good yields, leading to racemic mixtures of each compound. Next, the inhibitory activity against P. falciparum of 18 compounds were tested, founding six compounds with IC50 < 20 mu M. The most active of these compounds was 8c; however, their unsaturated derivative 7c was inactive. Then, a structure-activity relationship analysis was done, founding that focused LUMO lobe on the specific molecular zone is related to inhibitory activity against P. falciparum. Finally, we found a potential inhibition of lactate dehydrogenase by oxindole derivatives, using molecular docking virtual screening. (AU) | |
| FAPESP's process: | 13/07600-3 - CIBFar - Center for Innovation in Biodiversity and Drug Discovery |
| Grantee: | Glaucius Oliva |
| Support Opportunities: | Research Grants - Research, Innovation and Dissemination Centers - RIDC |
| FAPESP's process: | 17/26679-0 - 4-Quinolone derivatives as antimalarial drug candidates: Antiplasmodial activity characterization in vitro, in vivo and of the mode of action |
| Grantee: | Juliana Oliveira de Souza |
| Support Opportunities: | Scholarships in Brazil - Master |
| FAPESP's process: | 18/07287-7 - Discovery of Acridine and Marinoquinoline Derivatives as Plasmodium falciparum Inhibitors |
| Grantee: | Guilherme Eduardo de Souza |
| Support Opportunities: | Scholarships in Brazil - Doctorate |