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Synthesis and evaluation of phenylequine for antimalarial activity in vitro and in vivo.

Abstract：

:Synthesis of the potent antiplasmodial 4-aminoquinoline, phenylequine (PQ), is reported for the first time. PQ and the two analogues show increased efficacy in moving from the chloroquine sensitive D10 to the chloroquine resistant K1 strain in vitro. The in vivo efficacy of PQ, and salts thereof, have been determined in Plasmodium berghei ANKA and Plasmodium yoelii. Phenylequine hydrochloride has shown an ED(50) of 0.81 in P. yoelii (cf chloroquine ED(50)=1.31).

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Blackie MA,Yardley V,Chibale K

doi

10.1016/j.bmcl.2009.12.030

subject

Has Abstract

pub_date

2010-02-01 00:00:00

pages

1078-80

issue

3

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(09)01735-1

journal_volume

20

pub_type

杂志文章

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