长效且速效的体内有效抗疟氮杂环庚烷咔唑氨基醇
Long-Lasting and Fast-Acting in Vivo Efficacious Antiplasmodial Azepanylcarbazole Amino Alcohol.
作者信息
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
机构信息
Merck Global Health Institute, Ares Trading S.A., a subsidiary of Merck KGaA (Darmstadt, Germany), Coinsins 1267, Switzerland.
Medicines for Malaria Venture, 1215 Geneva, Switzerland.
出版信息
ACS Med Chem Lett. 2017 Nov 28;8(12):1304-1308. doi: 10.1021/acsmedchemlett.7b00391. eCollection 2017 Dec 14.
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.
摘要
2016年疟疾导致约42.9万人死亡，它仍然是一种主要的传染病，治疗发热症状以及提供相关的治疗后预防措施至关重要。本文公开了一种氮杂环庚烷基咔唑氨基醇，其在体内具有长效和快速起效的抗疟原虫功效，并且满足了理想的治疗后化学预防抗疟药物的众多特性。本文介绍了该化合物的合成、寄生虫学特征、动物药代动力学和药效学，并提出了一个潜在靶点。
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