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Long-Lasting and Fast-Acting in Vivo Efficacious Antiplasmodial Azepanylcarbazole Amino Alcohol
ACS Medicinal Chemistry Letters ( IF 4.2 ) Pub Date : 2017-12-06 00:00:00 , DOI: 10.1021/acsmedchemlett.7b00391
Nada Abla 1, 2 , Sridevi Bashyam 3 , Susan A. Charman , Béatrice Greco 1 , Philip Hewitt 4 , Maria Belén Jiménez-Díaz 5 , Kasiram Katneni , Holger Kubas 4 , Didier Picard 6 , Yuvaraj Sambandan 3 , Laura Sanz 5 , Dennis Smith , Tai Wang 6 , Paul Willis 2 , Sergio Wittlin 7, 8 , Thomas Spangenberg 1
Affiliation  

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.

中文翻译:

持久有效的体内有效抗疟原虫氮杂环戊烷咔唑氨基醇

疟疾在2016年有约429,000例死亡,仍然是一种主要的传染病,在这种情况下,治疗发热症状以及提供相关的治疗后预防措施至关重要。公开了一种具有长期和快速作用的体内抗疟药功效的氮杂环庚烷咔唑氨基醇,并满足所需的治疗后化学预防性抗疟药的许多属性。介绍了该化合物的合成,寄生虫学特征以及动物药代动力学和药效学,并提出了目标。
更新日期:2017-12-06
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