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Discovery of Potent and Fast-Acting Antimalarial Bis-1,2,4-triazines. 2021
Daniel L Priebbenow, and
Mitch Mathiew, and
Da-Hua Shi, and
Jitendra R Harjani, and
Julia G Beveridge, and
Marina Chavchich, and
Michael D Edstein, and
Sandra Duffy, and
Vicky M Avery, and
Robert T Jacobs, and
Stephen Brand, and
David M Shackleford, and
Wen Wang, and
Longjin Zhong, and
Given Lee, and
Erin Tay, and
Helena Barker, and
Elly Crighton, and
Karen L White, and
Susan A Charman, and
Amanda De Paoli, and
Darren J Creek, and
Jonathan B Baell
School of Chemistry, The University of Melbourne, Parkville, VIC 3010, Australia.
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, which exhibited significantly improved in vitro metabolic stability (8 and 42 μL/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.
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