Chemistry of Heterocyclic Compounds

, Volume 50, Issue 10, pp 1457–1463 | Cite as

Quinoxaline-Based Inhibitors of Malarial Protease PfSUB1*

  • S. S. Kher
  • M. Penzo
  • S. Fulle
  • J. P. Ebejer
  • P. W. Finn
  • M. J. Blackman
  • A. Jirgensons
Article

2,3-Bis(phenylamino)quinoxalines have been identified as a novel class of malarial protease PfSUB1 inhibitors by screening of Malaria Box compounds. The synthesis of analog series and investigation of their inhibitory activity provided preliminary structure–activity relationship to create in silico models for binding of these compounds into the active site of PfSUB1.

Keywords

quinoxaline inhibitors malaria Malaria Box PfSUB1 protease 

Notes

This work was supported by the EC Marie Curie Initial Training Network “Scientific Training in Antimicrobial Research Strategies” (grant agreement 238490).

The Malaria Box compound collection from Medicines for Malaria Venture foundation is gratefully acknowledged.

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Copyright information

© Springer Science+Business Media New York 2014

Authors and Affiliations

  • S. S. Kher
    • 1
  • M. Penzo
    • 2
  • S. Fulle
    • 3
    • 4
  • J. P. Ebejer
    • 3
  • P. W. Finn
    • 3
  • M. J. Blackman
    • 2
  • A. Jirgensons
    • 1
  1. 1.Latvian Institute of Organic SynthesisRigaLatvia
  2. 2.Division of ParasitologyMRC National Institute for Medical ResearchLondonU.K.
  3. 3.InhibOx Ltd., Oxford Centre for InnovationOxfordU.K.
  4. 4.BioMed X Innovation CenterHeidelbergGermany

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