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1.
Nat Prod Res ; 36(15): 3887-3893, 2022 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-33703954

RESUMO

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 H2/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 µM. 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.


Assuntos
Antimaláricos , Antimaláricos/farmacologia , Simulação de Acoplamento Molecular , Estrutura Molecular , Oxindóis/farmacologia , Plasmodium falciparum , Relação Estrutura-Atividade
2.
Asian Pac J Trop Biomed ; 1(1): 81-2, 2011 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-23569731

RESUMO

Cutaneous larva migrans (CLM) represents the most common tropically acquired dermatosis. CLM is caused by infection with hookworm larvae in tropical and sub-tropical areas, and people who have a history of foreign travel and of walking barefoot on sandy soil or beaches are at a high risk of getting infected with it. The diagnosis is usually made on the basis of the typical appearance of the lesion, intense itching and history of foreign travel. CLM is a common parasitic skin disease that can be easily prevented by wearing 'protective' footwear. A case of CLM is described in this article.


Assuntos
Larva Migrans , Adulto , Albendazol/uso terapêutico , Antinematódeos/uso terapêutico , Argentina , Brasil , Feminino , Humanos , Viagem
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