Synthesis and structure-activity relationships of antimalarial 4-oxo-3-carboxyl quinolones

Yiqun Zhang, W. Armand Guiguemde, Martina Sigal, Fangyi Zhu, Michele C. Connelly, Solomon Nwaka, R. Kiplin Guy

Research output: Contribution to journalArticlepeer-review

40 Scopus citations


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.

Original languageEnglish
Pages (from-to)2756-2766
Number of pages11
JournalBioorganic and Medicinal Chemistry
Issue number7
StatePublished - Apr 1 2010

Bibliographical note

Funding Information:
We thank Jean-Marc Paris and Allan Reitz for helpful discussions during the course of these studies. This work was funded by World Health Organization Grant 180738010 , the American Lebanese Syrian Associated Charities (ALSAC) , and St. Jude Children’s Research Hospital .


  • Malaria
  • Plasmodium
  • Quinolones
  • Synthesis

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry


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