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

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 ef...

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Veröffentlicht in:ACS medicinal chemistry letters 2017-12, Vol.8 (12), p.1304-1308
Hauptverfasser: Abla, Nada, Bashyam, Sridevi, Charman, Susan A, Greco, Béatrice, Hewitt, Philip, Jiménez-Díaz, Maria Belén, Katneni, Kasiram, Kubas, Holger, Picard, Didier, Sambandan, Yuvaraj, Sanz, Laura, Smith, Dennis, Wang, Tai, Willis, Paul, Wittlin, Sergio, Spangenberg, Thomas
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Sprache:eng
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Zusammenfassung: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.
ISSN:1948-5875
1948-5875
DOI:10.1021/acsmedchemlett.7b00391