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Author(s): Joana Matos
Filipa P da Cruz
Elia Cabrita
Jiri Gut
Fatima Nogueira
Virgilio E do Rosario
Rui Moreira
Philip J Rosenthal
Miguel Prudencio
Paula Gomes
Title: Novel Potent Metallocenes against Liver Stage Malaria
Issue Date: 2012
Abstract: 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.
Subject: Medicina básica
Basic medicine
Scientific areas: Ciências médicas e da saúde::Medicina básica
Medical and Health sciences::Basic medicine
Document Type: Artigo em Revista Científica Internacional
Rights: openAccess
Appears in Collections:FCUP - Artigo em Revista Científica Internacional

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