抗疟臭氧烷（OZ277）的构效关系。
The structure-activity relationship of the antimalarial ozonide arterolane (OZ277).
机构信息
College of Pharmacy, University of Nebraska Medical Center, 986025 Nebraska Medical Center, Omaha, NE, USA.
出版信息
J Med Chem. 2010 Jan 14;53(1):481-91. doi: 10.1021/jm901473s.
PMID:19924861
Abstract
The structure and stereochemistry of the cyclohexane substituents of analogues of arterolane (OZ277) had little effect on potency against Plasmodium falciparum in vitro. Weak base functional groups were not required for high antimalarial potency, but they were essential for high antimalarial efficacy in P. berghei-infected mice. Five new ozonides with antimalarial efficacy and ADME profiles superior or equal to that of arterolane were identified.
摘要
类似物（OZ277）中环己烷取代基的结构和立体化学对体外抗疟原虫活性影响不大。高效抗疟活性并不需要弱碱性官能团，但它们对感染伯氏疟原虫的小鼠的高效抗疟活性是必不可少的。鉴定出了 5 种具有抗疟疗效和 ADME 谱优于或等同于阿托烷的新臭氧化物。
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