Cyclopentane-based human NK1 antagonists. Part 2: Development of potent, orally active, water-soluble derivatives

Bioorganic & Medicinal Chemistry Letters(2006)

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摘要
The optimization of a cyclopentane-based hNK1 antagonist scaffold will be discussed in the context of enhanced water-solubility, sub-nanomolar hNK1 binding affinity, and oral activity in two in vivo models.
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关键词
Neurokinin-1: substance P,NK1 antagonist: cyclopentane-based structure
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