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

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.

SUBMITTER: Abla N

PROVIDER: S-EPMC5733276 | biostudies-literature | 2017 Dec

REPOSITORIES: biostudies-literature

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

Abla Nada N Bashyam Sridevi S Charman Susan A SA Greco Béatrice B Hewitt Philip P Jiménez-Díaz Maria Belén MB Katneni Kasiram K Kubas Holger H Picard Didier D Sambandan Yuvaraj Y Sanz Laura L Smith Dennis D Wang Tai T Willis Paul P Wittlin Sergio S Spangenberg Thomas T

ACS medicinal chemistry letters 20171128 12

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 pharmaco ...[more]

PMID: 29259752

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