Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 17, Issue 1, Pages 222-234Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2008.11.005
Keywords
Quinazoline; Antimalarial; Urea; In vitro; In vivo; P. falciparum
Funding
- CSIR, New Delhi
- ICMR, New Delhi
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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 IC50 of 16 compounds which have displayed MIC of 0.25 mu g/mL were also recorded. One of the compounds (24g) had IC50 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 (30g) displaying 40% curative activity (28 days) against mdr P. yoeilli nigeriensis at an oral dose of 100 mg/kg x 4days. (c) 2008 Elsevier Ltd. All rights reserved.
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