Journal
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY
Volume 56, Issue 3, Pages 1564-1570Publisher
AMER SOC MICROBIOLOGY
DOI: 10.1128/AAC.05345-11
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Funding
- Fundacao para a Ciencia e a Tecnologia (FCT) (Portugal)
- European Union [PTDC-QUI-65142-2006, FCOMP-01-0124-FEDER-007418, PTDC-BIA-BCM-71920-2006]
- FCT [CONC/REEQ/275/Qui, REDE/1517/RMN/2005]
- Fundação para a Ciência e a Tecnologia [PTDC/BIA-BCM/71920/2006] Funding Source: FCT
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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.
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