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α-Methylation at benzylic fragment of N-aryl-N′-benzyl ureas provides TRPV1 antagonists with better pharmacokinetic properties and higher efficacy in inflammatory …

A Gomtsyan, EK Bayburt, R Keddy, SC Turner…

文献索引:Bioorganic and Medicinal Chemistry Letters, , vol. 17, # 14 p. 3894 - 3899

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被引用次数: 23

摘要

... Bioorganic & Medicinal Chemistry Letters. ... The lack of correlation between in vitro and in vivo activities for 1 and (R)-16a can be explained by better pharmacokinetic properties of (R)-16a compared with 1. The most notable differences were larger volume of distribution (2.9 vs ...