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

doi:10.1021/acsmedchemlett.7b00391

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

Centre for Drug Candidate Optimisation

Research output: Contribution to journal › Article › Research › peer-review

12 Citations (Scopus)

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 language	English
Pages (from-to)	1304-1308
Number of pages	5
Journal	ACS Medicinal Chemistry Letters
Volume	8
Issue number	12
DOIs	https://doi.org/10.1021/acsmedchemlett.7b00391
Publication status	Published - 14 Dec 2017

Keywords

amino alcohol
Antiplasmodial
carbazole
Hsp90
pharmacodynamics
pharmacokinetics

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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Abla, N., Bashyam, S., Charman, S. A., Greco, B., Hewitt, P., Jiménez-Díaz, M. B., 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, 8(12), 1304-1308. https://doi.org/10.1021/acsmedchemlett.7b00391

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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

TY - JOUR

T1 - Long-Lasting and Fast-Acting in Vivo Efficacious Antiplasmodial Azepanylcarbazole Amino Alcohol

AU - Abla, Nada

AU - Bashyam, Sridevi

AU - Charman, Susan A.

AU - Greco, Béatrice

AU - Hewitt, Philip

AU - Jiménez-Díaz, Maria Belén

AU - Katneni, Kasiram

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

PY - 2017/12/14

Y1 - 2017/12/14

N2 - 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.

AB - 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.

KW - amino alcohol

KW - Antiplasmodial

KW - carbazole

KW - Hsp90

KW - pharmacodynamics

KW - pharmacokinetics

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U2 - 10.1021/acsmedchemlett.7b00391

DO - 10.1021/acsmedchemlett.7b00391

M3 - Article

AN - SCOPUS:85038355663

SN - 1948-5875

VL - 8

SP - 1304

EP - 1308

JO - ACS Medicinal Chemistry Letters

JF - ACS Medicinal Chemistry Letters

IS - 12

ER -

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

Abstract

Keywords

UN SDGs

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