《Discovery of Potent and Fast-Acting Antimalarial Bis-1,2,4-triazines》 was written by Priebbenow, Daniel L.; Mathiew, Mitch; Shi, Da-Hua; Harjani, Jitendra R.; Beveridge, Julia G.; Chavchich, Marina; Edstein, Michael D.; Duffy, Sandra; Avery, Vicky M.; Jacobs, Robert T.; Brand, Stephen; Shackleford, David M.; Wang, Wen; Zhong, Longjin; Lee, Given; Tay, Erin; Barker, Helena; Crighton, Elly; White, Karen L.; Charman, Susan A.; De Paoli, Amanda; Creek, Darren J.; Baell, Jonathan B.. Category: alcohols-buliding-blocks And the article was included in Journal of Medicinal Chemistry on April 8 ,2021. The article conveys some information:
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. The results came from multiple reactions, including the reaction of 3,3,3-Trifluoropropan-1-ol(cas: 2240-88-2Category: alcohols-buliding-blocks)
3,3,3-Trifluoropropan-1-ol(cas: 2240-88-2) is a important organic intermediate. It can be used in agrochemical, pharmaceutical and dyestuff field.Category: alcohols-buliding-blocks
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