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

28 Nov 2017

Nada Abla, Sridevi Bashyam, Susan A. Charman, Béatrice Greco, Philip Hewitt, Maria Belén Jiménez-Díaz, Kasiram Katneni, Holger Kubas, Didier Picard, Yuvaraj Sambandan, Laura Sanz, Dennis Smith, Tai Wang, Paul Willis, Sergio Wittlin, and Thomas Spangenberg

ACS Medicinal Chemistry Letters

DOI: 10.1021/acsmedchemlett.7b00391

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.

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