2-aryl indole NK1 receptor antagonists:: Optimisation of the 2-aryl ring and the indole nitrogen substituent

被引：50

作者：

Dinnell, K

Chicchi, GG

Dhar, MJ

Elliott, JM

Hollingworth, GJ

Kurtz, MM

Ridgill, MP

Rycroft, W

Tsao, KL

Williams, AR

Swain, CJ

机构：

[1] Merck Sharp & Dohme Res Labs, Neurosci Res Ctr, Dept Med Chem, Harlow CM20 2QR, Essex, England

[2] Merck Sharp & Dohme Res Labs, Neurosci Res Ctr, Dept Pharmacol, Harlow CM20 2QR, Essex, England

[3] Merck Res Labs, Dept Med Chem, Rahway, NJ 07065 USA

[4] Merck Res Labs, Dept Biochem, Rahway, NJ 07065 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 09期

关键词：

D O I：

10.1016/S0960-894X(01)00183-4

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Novel 2-aryl indole hNK(1) receptor ligands were prepared utilising palladium cross-coupling chemistry of a late intermediate as a key step. Compounds with high hNK(1) receptor binding affinity and good brain penetration (e.g., 9d) were synthesised. (C) 2001 Elsevier Science Ltd. All rights reserved.

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页码：1237 / 1240

页数：4

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