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J Med Chem. 2007 Jan 25;50(2):394-8.

Synthesis and antimalarial activity of side chain modified 4-aminoquinoline derivatives.

Author information

1
Division of Medicinal and Process Chemistry, Central Drug Research Institute, Lucknow 226 001, India.

Abstract

A new series of side-chain modified 4-aminoquinolines have been synthesized and found active against P. falciparum in vitro and P. yoelli in vivo. Compounds 6, 11, 12, and 19 exhibited superior in vitro activity compared to chloroquine. Selected compounds 6, 12, and 19 exhibited significant suppression in the in vivo assay. These analogs form a complex with hematin and inhibit the beta-hematin formation, suggesting that this class of compounds act on a heme polymerization target.

PMID:
17228883
DOI:
10.1021/jm061002i
[Indexed for MEDLINE]

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