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Novel squaramides with in vitro liver stage antiplasmodial activity.

Abstract：

:A structure-activity relationship study was performed with ten 8-aminoquinoline-squaramides compounds active against liver stage malaria parasites, using human hepatoma cells (Huh7) infected by Plasmodium berghei parasites. In addition, their blood-schizontocidal activity was assessed against chloroquine-resistant W2 strain Plasmodium falciparum. Compound 3 was 7.3-fold more potent than the positive control primaquine against liver-stage parasites, illustrating the importance of the squarate moiety to activity.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Ribeiro CJ,Espadinha M,Machado M,Gut J,Gonçalves LM,Rosenthal PJ,Prudêncio M,Moreira R,Santos MM

doi

10.1016/j.bmc.2016.03.005

subject

Has Abstract

pub_date

2016-04-15 00:00:00

pages

1786-92

issue

8

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(16)30142-0

journal_volume

24

pub_type

杂志文章

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