Article
Preclinical evaluation of the antifolate QN254, 5-chloro- N'6'-(2,5-dimethoxy-benzyl)-quinazoline-2,4,6-triamine, as an antimalarial drug candidate.
Antimicrobial agents and chemotherapy - 1 Jun 2010
Nzila Alexis, Rottmann Matthias, Chitnumsub Penchit, Kiara Stevens M, Kamchonwongpaisan Sumalee, Maneeruttanarungroj Cherdsak, Taweechai Supannee, Yeung Bryan K S, Goh Anne, Lakshminarayana Suresh B, Zou Bin, Wong Josephine, Ma Ngai Ling, Weaver Margaret, Keller Thomas H, Dartois Veronique, Wittlin Sergio, Brun Reto, Yuthavong Yongyuth, Diagana Thierry T
Abstract excerpt
Drug resistance against dihydrofolate reductase (DHFR) inhibitors-such as pyrimethamine (PM)-has now spread to almost all regions where malaria is endemic, rendering antifolate-based malaria treatments highly ineffective. We have previously shown that the di-amino quinazoline QN254 [5-chloro-N'6'-(2,5-dimethoxy-benzyl)-quinazoline-2,4,6-triamine] is active against the highly PM-resistant Plasmodium falciparum V1S...
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