4.7 Article

Synthesis of 2,4,6-trisubstituted pyrimidines as antimalarial agents

Journal

BIOORGANIC & MEDICINAL CHEMISTRY
Volume 13, Issue 15, Pages 4645-4650

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2005.04.061

Keywords

dihydrofolate reductase; antimalarial; pyrimidine

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A series of 2,4,6-trisubstituted-pyrimidines were synthesized and evaluated for their in vitro antimalarial activity against Plasmodium falciparum. Of the 18 compounds synthesized, 14 compounds have shown MIC in the range of 0.25-2 mu g/mL. These compounds are in vitro severalfold more active than pyrimethamine. (c) 2005 Elsevier Ltd. All rights reserved.

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