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Metallocene-based antimalarials: an exploration into the influence of the ferrocenyl moiety on in vitro antimalarial activity in chloroquine-sensitive and chloroquine-resistant strains of Plasmodium falciparum.

Abstract：

:To establish the role of the ferrocenyl moiety in the antiplasmodial activity of ferroquine, compounds in which this moiety is replaced by the corresponding ruthenium-based moieties were synthesized and evaluated. In both the sensitive (D10) and resistant (K1) strains of Plasmodium falciparum, ruthenoquine analogues showed comparable potency to ferroquine. This suggests that a probable role of the ferrocenyl fragment is to serve simply as a hydrophobic spacer group. In addition, ferroquine analogues with different aromatic substituents were synthesized and evaluated. Unexpectedly high activity for quinoline compounds lacking the 7-chloro substituent suggests the ferrocenyl moiety may have an additive and/or synergistic effect.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Blackie MA,Beagley P,Croft SL,Kendrick H,Moss JR,Chibale K

doi

10.1016/j.bmc.2007.07.012

subject

Has Abstract

pub_date

2007-10-15 00:00:00

pages

6510-6

issue

20

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(07)00628-1

journal_volume

15

pub_type

杂志文章

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