Silveira, Flavia F. published the artcileComparative study between the anti-P. falciparum activity of triazolopyrimidine, pyrazolopyrimidine and quinoline derivatives and the identification of new PfDHODH inhibitors, Recommanded Product: 7-Chloro-5-methyl-[1,2,4]triazolo[1,5-a]pyrimidine, the main research area is triazolopyrimidine derivative preparation antimalarial PfDHODH inhibitor; pyrazolopyrimidine derivative preparation antimalarial PfDHODH inhibitor; quinoline derivative preparation antimalarial PfDHODH inhibitor; Malaria; P. falciparum; PfDHODH; Pyrazolopyrimidine; Quinoline; Triazolopyrimidine.
Three series of triazolopyrimidine I [R = H, Me, CF3; R1 = Ph, 4-MeC6H4, 4-ClC6H4, etc.], pyrazolopyrimidine II [R2 = Ph, 4-MeOC6H4, 4-FC6H4, etc.] and quinoline derivatives III [R3 = Ph, 2-naphthyl, 4-ClC6H4, etc.] as P. falciparum inhibitors (3D7 strain) was reported. Some of the compounds of I, II and III exhibited anti-P. falciparum activity, with IC50 values ranging from 0.030 to 9.1μM. Compounds I were more potent than the compounds II and III. Compounds I [R = CF3; R1 = 2-naphthyl, 4-MeC6H4, 4-FC6H4, 4-F3CC6H4] were the most potent inhibitors, with IC50 values in the range of 0.030-0.086μM and were equipotent to chloroquine. In addition, the compounds were selective, showed no cytotoxic activity against the human hepatoma cell line HepG2. All compounds I inhibited PfDHODH activity in the low micromolar to low nanomolar range (IC50 values of 0.08-1.3μM) and did not show significant inhibition against the HsDHODH homolog (0-30% at 50μM). Mol. docking studies indicated the binding mode of compounds I to PfDHODH and the highest interaction affinities for the PfDHODH enzyme were in agreement with the in vitro exptl. evaluation. Thus, the most active compounds against P. falciparum parasites I [R = CF3; R1 = 4-MeC6H4, 4-FC6H4, 4-F3CC6H4, 2-naphthyl] (IC50 = 0.086μM, 0.032μM, 0.030μM, 0.050μM, resp.) and the most active inhibitor against PfDHODH I [R = CF3; R1 = 4-ClC6H4] (IC50 = 0.08μM – PfDHODH) stood out as new lead compounds for antimalarial drug discovery. Their potent in vitro activity against P. falciparum and the selective inhibition of the PfDHODH enzyme strongly suggested that this was the mechanism of action underlying this series of compounds I.
European Journal of Medicinal Chemistry published new progress about Acids Role: RCT (Reactant), RACT (Reactant or Reagent). 24415-66-5 belongs to class triazoles, name is 7-Chloro-5-methyl-[1,2,4]triazolo[1,5-a]pyrimidine, and the molecular formula is C6H5ClN4, Recommanded Product: 7-Chloro-5-methyl-[1,2,4]triazolo[1,5-a]pyrimidine.
Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics