Parallel synthesis and antimalarial screening of a 4-aminoquinoline library

Peter B. Madrid, Nathan T. Wilson, Joseph L. DeRisi, R. Kiplin Guy

Research output: Contribution to journalArticlepeer-review

64 Scopus citations


Due to growing problems with drug resistance, there is an outstanding need for new, cost-effective drugs for the treatment of malaria. The 4-aminoquinolines have provided a number of useful antimalarials, and Plasmodium falciparum, the causative organism for the most deadly form of human malaria, is generally slow to develop resistance to these drugs. Therefore, diverse screening libraries of quinolines continue to be useful for antimalarial drug discovery. We report herein the development of an efficient method for producing libraries of 4-aminoquinolines variant in the side chain portion of the molecule. The effects of these substitutions were evaluated by screening this library for activity against P. falciparum, revealing four potent compounds active against drug-resistant strains.

Original languageEnglish
Pages (from-to)437-442
Number of pages6
JournalJournal of Combinatorial Chemistry
Issue number3
StatePublished - May 2004

ASJC Scopus subject areas

  • Chemistry (all)


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