Discovery and optimisation studies of antimalarial phenotypic hits

Alka Mital, Dinakaran Murugesan, Marcel Kaiser, Clive Yeates, Ian H. Gilbert (Lead / Corresponding author)

Research output: Contribution to journalArticlepeer-review

13 Citations (Scopus)

Abstract

There is an urgent need for the development of new antimalarial compounds. As a result of a phenotypic screen, several compounds with potent activity against the parasite Plasmodium falciparum were identified. Characterization of these compounds is discussed, along with approaches to optimise the physicochemical properties. The in vitro antimalarial activity of these compounds against P. falciparum K1 had EC50 values in the range of 0.09e29 mM, and generally good selectivity (typically >100-fold) compared to a mammalian cell line (L6). One example showed no significant activity against a rodent model of malaria, and more work is needed to optimise these compounds.

Original languageEnglish
Pages (from-to)530-538
Number of pages9
JournalEuropean Journal of Medicinal Chemistry
Volume103
DOIs
Publication statusPublished - 20 Oct 2015

Keywords

  • Malaria
  • Medicinal chemistry
  • Phenotypic hit
  • Plasmodium falciparum

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