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Title

Long-Lasting and Fast-Acting in Vivo Efficacious Antiplasmodial Azepanylcarbazole Amino Alcohol

Authors
Bashyam, Sridevi
Charman, Susan A.
Greco, Béatrice
Hewitt, Philip
Jiménez-Díaz, Maria Belén
Katneni, Kasiram
Kubas, Holger
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Published in ACS Medicinal Chemistry Letters. 2017, vol. 8, no. 12, p. 1304-1308
Abstract With ∼429,000 deaths in 2016, malaria remains a major infectious disease where the need to treat the fever symptoms, but also to provide relevant post-treatment prophylaxis, is of major importance. An azepanylcarbazole amino alcohol is disclosed with a long- and fast-acting in vivo antiplasmodial efficacy and meets numerous attributes of a desired post-treatment chemoprophylactic antimalarial agent. The synthesis, the parasitological characterization, and the animal pharmacokinetics and pharmacodynamics of this compound are presented along with a proposed target.
Keywords Amino alcoholAntiplasmodialCarbazoleHsp90PharmacodynamicsPharmacokinetics
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Research group Groupe Picard
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ABLA, Nada et al. Long-Lasting and Fast-Acting in Vivo Efficacious Antiplasmodial Azepanylcarbazole Amino Alcohol. In: ACS Medicinal Chemistry Letters, 2017, vol. 8, n° 12, p. 1304-1308. https://archive-ouverte.unige.ch/unige:100460

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Deposited on : 2017-12-18

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