1266246-39-2Relevant academic research and scientific papers
Design, synthesis and biological evaluation of 6-aryl-1,6-dihydro-1,3,5-triazine-2,4-diamines as antiplasmodial antifolates
Lourens, Anna C. U.,Gravestock, David,Van Zyl, Robyn L.,Hoppe, Heinrich C.,Kolesnikova, Natasha,Taweechai, Supannee,Yuthavong, Yongyuth,Kamchonwongpaisan, Sumalee,Rousseau, Amanda L.
, p. 7899 - 7911 (2016/08/30)
The design, synthesis and biological evaluation of a series of 6-aryl-1,6-dihydro-1,3,5-triazine-2,4-diamines is described. These compounds exhibited in vitro antiplasmodial activity in the low nanomolar range against both drug sensitive and drug resistant strains of P. falciparum, with 1-(3-(2,4-dichlorophenoxy)propyl)-6-phenyl-1,6-dihydro-1,3,5-triazine-2,4-diamine hydrochloride identified as the most potent compound from this series against the drug resistant FCR-3 strain (IC50 2.66 nM). The compounds were not toxic to mammalian cells at therapeutic concentrations and were shown to be inhibitors of parasitic DHFR in a biochemical enzyme assay.
TRIAZINE DERIVATES FOR USE IN THE TREATMENT OF MALARIA
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Page/Page column 18-19, (2011/02/24)
The invention provides compounds of formula (I), in which R1 and R2 are independently selected from H, alkyl, aryl and heteroaryl, or R1 and R2 together form a C5-C7 ring, R3-R7 are independently selected from H, halogen, alkyl and alkoxy, X is (CH2)n in which n is 0-5, Y is selected from CH2, NR8, O or S in which R8 is H or alkyl, salts thereof and stereoisomers thereof, for the prophylaxis or treatment of malaria.
