Identification and chemical synthesis of MDL 105,212, a non-peptide tachykinin antagonist with high affinity for NK1 and NK2 receptors.

被引：28

作者：

Burkholder, TP

Kudlacz, EM

Le, TB

Knippenberg, RW

Shatzer, SA

Maynard, GD

Webster, ME

Horgan, SW

机构：

[1] Hoechst Marion Roussel, Cincinnati, OH 45215

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1996年 / 6卷 / 08期

关键词：

D O I：

10.1016/0960-894X(96)00148-5

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We have synthesized and identified MDL 105,212, a non-peptide tachykinin receptor antagonist that has high affinity for human NK1 (IC50=3.11 nM) and NK2 (IC50=8.40 nM) receptors. The chemical synthesis of MDL 105,212 and the SAR of a series of racemic amide analogs are described. Copyright (C) 1996 Elsevier Science Ltd

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页码：951 / 956

页数：6

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