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Synthesis and antimalarial activity of 2-guanidino-4-oxoimidazoline derivatives.

Abstract：

:A series of 2-guanidino-4-oxoimidazoline (deoxo-IZ) derivatives was prepared and showed potent antimalarial activities in rodent and Rhesus models. Compound 8e, the most potent analogues of this series, is the first non-8-aminoqinoline antimalarial that demonstrated radical curative activity in non-human primate by oral route and showed causal prophylactic activity comparable to that of the commonly used clinical drugs in Rhesus monkeys infected with sporozoites of Plasmodium cynomolgi. The metabolic stability and metabolites profile indicated that the new deoxo-IZ derivatives (8) may act as prodrugs of the corresponding IZ (1 and 2) derivatives.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Liu X,Wang X,Li Q,Kozar MP,Melendez V,O'Neil MT,Lin AJ

doi

10.1021/jm200111g

subject

Has Abstract

pub_date

2011-07-14 00:00:00

pages

4523-35

issue

13

eissn

0022-2623

issn

1520-4804

journal_volume

54

pub_type

杂志文章

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