Long-lasting and fast-acting in vivo efficacious antiplasmodial azepanylcarbazole amino alcohol
Date Issued
2017-01-01
Author(s)
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
Spangenberg, Thomas
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.