Hameed P, Shahul published the artcileAminoazabenzimidazoles, a Novel Class of Orally Active Antimalarial Agents, Category: triazoles, the main research area is aminoazabenzimidazole preparation SAR antimalarial Plasmodium.
Whole-cell high-throughput screening of the AstraZeneca compound library against the asexual blood stage of Plasmodium falciparum (Pf) led to the identification of amino imidazoles, a robust starting point for initiating a hit-to-lead medicinal chem. effort. Structure-activity relation studies followed by pharmacokinetics optimization resulted in the identification of (I) as an attractive lead with good oral bioavailability. Compound I was efficacious (ED90 of 28.6 mg·kg-1) in the humanized P. falciparum mouse model of malaria (Pf/SCID model). Representative compounds displayed a moderate to fast killing profile that is comparable to that of chloroquine. This series demonstrates no cross-resistance against a panel of Pf strains with mutations to known antimalarial drugs, thereby suggesting a novel mechanism of action for this chem. class.
Journal of Medicinal Chemistry published new progress about Antimalarials. 502546-41-0 belongs to class triazoles, name is 5-Cyclopropyl-4H-1,2,4-triazol-3-amine, and the molecular formula is C5H8N4, Category: triazoles.
Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics