Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 18, Issue 7, Pages 2756-2766Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2010.02.013
Keywords
Malaria; Quinolones; Plasmodium; Synthesis
Funding
- World Health Organization [180738010]
- American Lebanese Syrian Associated Charities (ALSAC)
- St. Jude Children's Research Hospital
- NATIONAL INSTITUTE OF ALLERGY AND INFECTIOUS DISEASES [U01AI075517] Funding Source: NIH RePORTER
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Malaria is endemic in tropical and subtropical regions of Africa, Asia, and the Americas. The increasing prevalence of multi-drug-resistant Plasmodium falciparum drives the ongoing need for the development of new antimalarial drugs. In this light, novel scaffolds to which the parasite has not been exposed are of particular interest. Recently, workers at the Swiss Tropical Institute discovered two novel 4-oxo-3-carboxyl quinolones active against the intra-erythrocytic stages of P. falciparum while carrying out rationally directed low-throughput screening of potential antimalarial agents as part of an effort directed by the World Health Organization. Here we report the design, synthesis, and preliminary pharmacologic characterization of a series of analogues of 4-oxo-3-carboxyl quinolones. These studies indicate that the series has good potential for preclinical development. (C) 2010 Elsevier Ltd. All rights reserved.
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