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4-Aminoquinoline derived antimalarials: synthesis, antiplasmodial activity and heme polymerization inhibition studies.

Abstract：

:A new series of 4-aminoquinoline derivatives have been synthesized and found to be active against both susceptible and resistant strains of Plasmodium falciparum in vitro. Compound 1-[3-(7-chloro-quinolin-4-ylamino)-propyl]-3-cyclopropyl-thiourea (7) exhibited superior in vitro activity against resistant strains of P. falciparum as compared to chloroquine (CQ). All the compounds showed resistance factor between 0.59 and 4.31 as against 5.05 for CQ. Spectroscopic studies suggested that this class of compounds act on heme polymerization target.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Solomon VR,Haq W,Smilkstein M,Srivastava K,Puri SK,Katti SB

doi

10.1016/j.ejmech.2010.07.068

subject

Has Abstract

pub_date

2010-11-01 00:00:00

pages

4990-6

issue

11

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(10)00569-6

journal_volume

45

pub_type

杂志文章

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