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Search for new pharmacophores for antimalarial activity. Part II: synthesis and antimalarial activity of new 6-ureido-4-anilinoquinazolines.

Abstract：

:Synthesis of new 6-ureido-4-anilinoquinazolines have been accomplished and their in vitro antimalarial activity against chloroquine-sensitive P. falciparum have been examined. Out of 64 compounds evaluated, the IC(50) of 16 compounds which have displayed MIC of 0.25 microg/mL were also recorded. One of the compounds (24 g) had IC(50) value of 2.27 ng/mL which was equipotent to the standard drug chloroquine used in the bioassay. The in vivo evaluation of a few compounds among the series led to discovery of one analog (30 g) displaying 40% curative activity (28 days) against mdr P. yoeillinigeriensis at an oral dose of 100 mg/kg x 4 days.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Madapa S,Tusi Z,Mishra A,Srivastava K,Pandey SK,Tripathi R,Puri SK,Batra S

doi

10.1016/j.bmc.2008.11.005

subject

Has Abstract

pub_date

2009-01-01 00:00:00

pages

222-34

issue

1

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(08)01064-X

journal_volume

17

pub_type

杂志文章

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