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

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, Thomas Spangenberg

Research output: Contribution to journalArticleResearchpeer-review

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.

Original languageEnglish
Pages (from-to)1304-1308
Number of pages5
JournalACS Medicinal Chemistry Letters
Volume8
Issue number12
DOIs
Publication statusPublished - 14 Dec 2017

Keywords

  • amino alcohol
  • Antiplasmodial
  • carbazole
  • Hsp90
  • pharmacodynamics
  • pharmacokinetics

Cite this

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. / Long-Lasting and Fast-Acting in Vivo Efficacious Antiplasmodial Azepanylcarbazole Amino Alcohol. In: ACS Medicinal Chemistry Letters. 2017 ; Vol. 8, No. 12. pp. 1304-1308.
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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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Abla, N, Bashyam, S, Charman, SA, Greco, B, Hewitt, P, Jiménez-Díaz, MB, Katneni, K, Kubas, H, Picard, D, Sambandan, Y, Sanz, L, Smith, D, Wang, T, Willis, P, Wittlin, S & Spangenberg, T 2017, 'Long-Lasting and Fast-Acting in Vivo Efficacious Antiplasmodial Azepanylcarbazole Amino Alcohol' ACS Medicinal Chemistry Letters, vol. 8, no. 12, pp. 1304-1308. https://doi.org/10.1021/acsmedchemlett.7b00391

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

In: ACS Medicinal Chemistry Letters, Vol. 8, No. 12, 14.12.2017, p. 1304-1308.

Research output: Contribution to journalArticleResearchpeer-review

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AU - Greco, Béatrice

AU - Hewitt, Philip

AU - Jiménez-Díaz, Maria Belén

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AU - Kubas, Holger

AU - Picard, Didier

AU - Sambandan, Yuvaraj

AU - Sanz, Laura

AU - Smith, Dennis

AU - Wang, Tai

AU - Willis, Paul

AU - Wittlin, Sergio

AU - Spangenberg, Thomas

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