Novel Potent Metallocenes against Liver Stage Malaria

• Tipo: Artigo em Revista Científica Internacional
• Data: 2012

Autores

Joana Matos (Autor) Outra; Filipa P da Cruz (Autor) Outra; Elia Cabrita (Autor) Outra; Jiri Gut (Autor) Outra; Fatima Nogueira (Autor) Outra; Virgilio E do Rosario (Autor) Outra; Rui Moreira (Autor) Outra; Philip J Rosenthal (Autor) Outra; Miguel Prudencio (Autor) Outra; Paula Gomes (Autor) FCUP

Revista

Título: Antimicrobial Agents and Chemotherapy

Vol. 56

Páginas: 1564-1570

ISSN: 0066-4804

Editora: American Society for Microbiology

Indexação

ISI Web of Knowledge - 34 Citações

Scopus - 35 Citações

Classificação Científica

FOS: Ciências médicas e da saúde > Medicina básica

Outras Informações

ID Authenticus: P-002-CPH

DOI: 10.1128/aac.05345-11

Abstract (EN): Novel conjugates of the antimalarial drug primaquine (compound 1) with ferrocene, named primacenes, have been synthesized and screened for their activities against blood stage and liver stage malaria in vitro and host-vector transmission in vivo. Both transmission-blocking and blood-schizontocidal activities of the parent drug were conserved only in primacenes bearing a basic aliphatic amine group. Liver stage activity did not require this structural feature, and all metallocenes tested were comparable to or better than primaquine in this regard. Remarkably, the replacement of primaquine's aliphatic chain by hexylferrocene, as in compound 7, led to a similar to 45-fold-higher level activity against liver stage parasitemia than that of primaquine.

Idioma: Inglês

Tipo (Avaliação Docente): Científica