Synthesis of ring-substituted 4-aminoquinolines and evaluation of their antimalarial activities

Peter B. Madrid, John Sherrill, Ally P. Liou, Jennifer L. Weisman, Joseph L. DeRisi, R. Kiplin Guy

Research output: Contribution to journalArticlepeer-review

119 Scopus citations


A simple two-step synthesis method was used to make 51 B-ring-substituted 4-hydroxyquinolines allowing analysis of the effect of ring substitutions on inhibition of growth of chloroquine sensitive and resistant strains of Plasmodium falciparum, the dominant cause of malaria morbidity. Substituted quinoline rings other than the 7-chloroquinoline ring found in chloroquine were found to have significant activity against the drug-resistant strain of P. falciparum W2.

Original languageEnglish
Pages (from-to)1015-1018
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Issue number4
StatePublished - Feb 15 2005

Bibliographical note

Funding Information:
The Sandler Research Foundation and the NIH (AI053862).


  • 4-Aminoquinoline malaria

ASJC Scopus subject areas

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


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