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Younis, Yassir; Douelle, Frederic; Feng, Tzu-Shean; Cabrera, Diego González; Manach, Claire Le; Nchinda, Aloysius T; Duffy, Sandra; White, Karen L; Shackleford, David M; Morizzi, Julia; Mannila, Janne; Katneni, Kasiram; Bhamidipati, Ravi; Zabiulla, K. Mohammed; Joseph, Jayan T; Bashyam, Sridevi; Waterson, David; Witty, Michael J; Hardick, David; Wittlin, Sergio; Avery, Vicky; Charman, Susan A; Chibale, Kelly
Journal of medicinal chemistry, 04/2012, Letnik: 55, Številka: 7Journal Article
A novel class of orally active antimalarial 3,5-diaryl-2-aminopyridines has been identified from phenotypic whole cell high-throughput screening of a commercially available SoftFocus kinase library. The compounds were evaluated in vitro for their antiplasmodial activity against K1 (chloroquine and drug-resistant strain) and NF54 (chloroquine-susceptible strain) as well as for their cytotoxicity. Synthesis and structure–activity studies identified a number of promising compounds with selective antiplasmodial activity. One of these frontrunner compounds, 15, was equipotent across the two strains (K1 = 25.0 nM, NF54 = 28.0 nM) and superior to chloroquine in the K1 strain (chloroquine IC50 K1 = 194.0 nM). Compound 15 completely cured Plasmodium berghei-infected mice with a single oral dose of 30 mg/kg. Dose–response studies generated ED50 and ED90 values of 0.83 and 1.74 mg/kg for 15 in the standard four-dose Peters test. Pharmacokinetic studies in the rat indicated that this compound has good oral bioavailability (51% at 20 mg/kg) and a reasonable half-life (t 1/2 ∼ 7–8 h).
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JCR | SNIP | JCR | SNIP | JCR | SNIP | JCR | SNIP |
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