Novel potent metallocenes against liver stage malaria

Joana Matos, Filipa P. Da Cruz, Élia Cabrita, Jiri Gut, Fátima Nogueira, Virgílio E. Do Rosário, Rui Moreira, Philip J. Rosenthal, Miguel Prudêncio, Paula Gomes

Research output: Contribution to journalArticlepeer-review

32 Citations (Scopus)

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 ∼45-fold-higher level activity against liver stage parasitemia than that of primaquine.

Original languageEnglish
Pages (from-to)1564-1570
Number of pages7
JournalAntimicrobial Agents and Chemotherapy
Volume56
Issue number3
DOIs
Publication statusPublished - Mar 2012

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