92017-89-5Relevant articles and documents
Triazolopyrimidine-based dihydroorotate dehydrogenase inhibitors with potent and selective activity against the malaria parasite Plasmodium falciparum
Phillips, Margaret A.,Gujjar, Ramesh,Malmquist, Nicholas A.,White, John,El Mazouni, Farah,Baldwin, Jeffrey,Rathod, Pradipsinh K.
supporting information; experimental part, p. 3649 - 3653 (2009/04/07)
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 (EC 50 = 79 nM).
Reaction of 3-oxo-N-phenylbutanethioamide with 5-amino-1H-1,2,4-triazoles
Britsun,Borisevich,Samoilenko,Chernega,Lozinskii
, p. 1516 - 1520 (2007/10/03)
Reactions of 3-oxo-N-phenylbutanethioamide with 3-substituted 5-amino-1H-1,2,4-triazoles in acetic acid led to the formation of 5-methyl-7,8-dihydro[1,2,4]triazolo[1,5-a]pyrimidine-7-thiones, 7-methyl-5,8-dihydrol[1,2,4]triazolo[1,5-a]pyrimidine-5-thiones