The Structure-Activity Relationship of the Antimalarial Ozonide Arterolane (OZ277)
The Structure-Activity Relationship of the Antimalarial Ozonide Arterolane (OZ277)
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DOI：
10.1021/jm901473s
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发表时间：
2010-01-14
影响因子：
7.3
通讯作者：
Vennerstrom, Jonathan L.
中科院分区：
文献类型：
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作者：
Dong, Yuxiang;Wittlin, Sergio;Vennerstrom, Jonathan L.
大环戊烷类似物(OZ277)的环己烷取代基的结构和立体化学对体外抗菌活性影响不大。弱碱性官能团并不是高抗疟效力所必需的，但它们对于伯氏疟原虫感染小鼠的高抗疟效果是必不可少的。鉴定了五种新的臭氧化合物，它们的抗疟疾效果和ADME曲线优于或等于动脉戊烷。
The structure and stereochemistry of the cyclohexane substituents of analogues of arterolane (OZ277) had little effect on potency against 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.