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

• Tipo: Artigo em Revista Científica Internacional
• Data: 2015

Autores

Ana Gomes (Autor) Outra; Marta Machado (Autor) Outra; Lis Lobo (Autor) Outra; Fatima Nogueira (Autor) Outra; Miguel Prudencio (Autor) Outra; Catia Teixeira (Autor) Outra; Paula Gomes (Autor) FCUP

Revista

Título: ChemMedChem

Vol. 10

Páginas: 1344-1349

ISSN: 1860-7179

Editora: Wiley-Blackwell

Indexação

ISI Web of Knowledge - 12 Citações

Scopus - 13 Citações

Classificação Científica

FOS: Ciências médicas e da saúde > Medicina básica

Outras Informações

ID Authenticus: P-00G-E32

DOI: 10.1002/cmdc.201500164

Abstract (EN): 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 Plasmodiumspp. 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: Inglês

Tipo (Avaliação Docente): Científica