Spirocyclic NK1 antagonists I:: [4.5] and [5.5]-spiroketals

被引：25
作者：
Seward, EM
Carlson, E
Harrison, T
Haworth, KE
Herbert, R
Kelleher, FJ
Kurtz, MM
Moseley, J
Owen, SN
Owens, AP
Sadowski, SJ
Swain, CJ
Williams, BJ
机构：
[1] Merck Sharp & Dohme Res Labs, Dept Med Chem, Ctr Res Neurosci, Harlow, Essex, England
[2] Merck Sharp & Dohme Res Labs, Dept Pharmacol, Ctr Res Neurosci, Harlow, Essex, England
[3] Merck Res Labs, Dept Biochem, Rahway, NJ 07065 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 18期
关键词：
D O I：
10.1016/S0960-894X(02)00506-1
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of novel spiroketal-based NK1 antagonists is described. The effect of modifications to the spiroether ring and aromatic substituents are discussed, leading to the identification of compounds with high affinity and excellent CNS penetration. (C) 2002 Elsevier Science Ltd. All rights reserved.
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页码：2515 / 2518
页数：4
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