Priebbenow, Daniel L. published the artcileDiscovery of Potent and Fast-Acting Antimalarial Bis-1,2,4-triazines, Safety of 3,3,3-Trifluoropropan-1-ol, the publication is Journal of Medicinal Chemistry (2021), 64(7), 4150-4162, database is CAplus and MEDLINE.
Novel 3,3′-disubstituted-5,5′-bi(1,2,4-triazine) compounds with potent in vitro activity against Plasmodium falciparum parasites were recently discovered. To improve the pharmacokinetic properties of the triazine derivatives, a new structure-activity relationship (SAR) investigation was initiated with a focus on enhancing the metabolic stability of lead compounds These efforts led to the identification of second-generation highly potent antimalarial bis-triazines, exemplified by triazine 23(I), which exhibited significantly improved in vitro metabolic stability (8 and 42μL/min/mg protein in human and mouse liver microsomes). The disubstituted triazine dimer 23 was also observed to suppress parasitemia in the Peters 4-day test with a mean ED50 value of 1.85 mg/kg/day and exhibited a fast-killing profile, revealing a new class of orally available antimalarial compounds of considerable interest.
Journal of Medicinal Chemistry published new progress about 2240-88-2. 2240-88-2 belongs to alcohols-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Aliphatic hydrocarbon chain,Alcohol, name is 3,3,3-Trifluoropropan-1-ol, and the molecular formula is C3H5F3O, Safety of 3,3,3-Trifluoropropan-1-ol.
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