N-Cinnamoylation of Antimalarial Classics: Effects of Using Acyl Groups Other than Cinnamoyl toward Dual-Stage Antimalarials

Ana Gomes, Marta Machado, Lis Lobo, Fátima Nogueira, Miguel Prudêncio, Cátia Teixeira*, Paula Gomes

*Autor correspondente para este trabalho

Resultado de pesquisarevisão de pares

15 Citações (Scopus)

Resumo

In a follow-up study to our reports of N-cinnamoylated chloroquine and quinacrine analogues as promising dual-stage antimalarial leads with high in vitro potency against both blood-stage Plasmodium falciparum and liver-stage Plasmodium berghei, we decided to investigate the effect of replacing the cinnamoyl moiety with other acyl groups. Thus, a series of N-acylated analogues were synthesized, and their activities against blood- and liver-stage Plasmodium spp. were assessed along with their in vitro cytotoxicities. Although the new N-acylated analogues were found to be somewhat less active and more cytotoxic than their N-cinnamoylated counterparts, they equally displayed nanomolar activities in vitro against blood-stage drug-sensitive and drug-resistant P. falciparum, and significant in vitro liver-stage activity against P. berghei. Therefore, it is demonstrated that simple N-acylated surrogates of classical antimalarial drugs are promising dual-stage antimalarial leads.

Idioma originalEnglish
Páginas (de-até)1344-1349
Número de páginas6
RevistaChemMedChem
Volume10
Número de emissão8
DOIs
Estado da publicaçãoPublicado - 1 ago. 2015
Publicado externamenteSim

Impressão digital

Mergulhe nos tópicos de investigação de “N-Cinnamoylation of Antimalarial Classics: Effects of Using Acyl Groups Other than Cinnamoyl toward Dual-Stage Antimalarials“. Em conjunto formam uma impressão digital única.

Citação