2. Academic Validation
  3. Triazolopyrimidine-based dihydroorotate dehydrogenase inhibitors with potent and selective activity against the malaria parasite Plasmodium falciparum

Triazolopyrimidine-based dihydroorotate dehydrogenase inhibitors with potent and selective activity against the malaria parasite Plasmodium falciparum

  • J Med Chem. 2008 Jun 26;51(12):3649-53. doi: 10.1021/jm8001026.
Margaret A Phillips 1,  Ramesh Gujjar,  Nicholas A Malmquist,  John White,  Farah El Mazouni,  Jeffrey Baldwin,  Pradipsinh K Rathod
Affiliations

Affiliation

  • 1 Department of Pharmacology, University of Texas Southwestern Medical Center at Dallas, 6001 Forest Park Boulevard, Dallas, TX 75390-9041, USA. margaret.phillips@UTSouthwestern.edu
PMID: 18522386 DOI: 10.1021/jm8001026
Abstract

A Plasmodium falciparum Dihydroorotate Dehydrogenase ( PfDHODH) inhibitor that is potent ( KI = 15 nM) and species-selective (>5000-fold over the human enzyme) was identified by high-throughput screening. The substituted triazolopyrimidine and its structural analogues were produced by an inexpensive three-step synthesis, and the series showed good association between PfDHODH inhibition and Parasite toxicity. This study has identified the first nanomolar PfDHODH inhibitor with potent antimalarial activity in whole cells (EC50 = 79 nM).

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