2-styryl-pyridines and 2-(3,4-dihydro-naphthalen-2-yl)-pyridines as potent NR1/2B subtype selective NMDA receptor antagonists

被引：4

作者：

Buettelmann, B ^{[1
]}

Alanine, A

Bourson, A

Gill, R

Heitz, MP

Mutel, V

Pinard, E

Trube, G

Wyler, R

机构：

[1] F Hoffmann La Roche Ltd, Div Pharma, Discovery Chem, CH-4070 Basel, Switzerland

[2] F Hoffmann La Roche Ltd, Div Pharma, Preclin CNS Res, CH-4070 Basel, Switzerland

来源：

CHIMIA | 2004年 / 58卷 / 09期

关键词：

neurodegeneration; NMDA; NR1/2B antagonists; structure-activity relationship;

D O I：

10.2533/000942904777677579

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

A series of 2-styryl-pyridines and 2-(3,4-dihydro-naphthalen-2-yl)-pyridines was prepared and evaluated as NR1/2B subtype selective NMDA receptor antagonists. The SAR developed in this series resulted in the discovery of high affinity antagonists that are selective (vs. alpha(1) and M-1 receptors) and are active in vivo.

引用

页码：630 / 633

页数：4

共 22 条

[1] SYNTHESIS OF BIOLOGICAL MARKERS IN FOSSIL-FUELS .2. SYNTHESIS AND C-13 NMR-STUDIES OF SUBSTITUTED INDANS AND TETRALINS [J].

ADAMCZYK, M ;

WATT, DS ;

NETZEL, DA .

JOURNAL OF ORGANIC CHEMISTRY, 1984, 49 (22) :4226-4237

[2]

Avdeef A., 1993, APPL THEORY GUIDE PH

[3] Correlation between 5-HT7 receptor affinity and protection against sound-induced seizures in DBA/2J mice [J].

Bourson, A ;

Kapps, V ;

Zwingelstein, C ;

Rudler, A ;

Boess, FG ;

Sleight, AJ .

NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY, 1997, 356 (06) :820-826

[4] 4-(3,4-Dihydro-1H-isoquinolin-2yl)-pyridines and 4-(3,4-dihydro-1H-isoquinolin-2-yl)-quinolines as potent NR1/2B subtype selective NMDA receptor antagonists [J].

Büttelmann, B ;

Alanine, A ;

Bourson, A ;

Gill, R ;

Heitz, MP ;

Mutel, V ;

Pinard, E ;

Trube, G ;

Wyler, R .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2003, 13 (10) :1759-1762

[5] 2-(3,4-dihydro-1H-isoquinolin-2yl)-pyridin as a novel class of NR1/2B subtype selective NMDA receptor antagonists [J].

Büttelmann, B ;

Alanine, A ;

Bourson, A ;

Gill, R ;

Heitz, MP ;

Mutel, V ;

Pinard, E ;

Trube, G ;

Wyler, R .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2003, 13 (05) :829-832

[6]

Chazot P L, 2000, Curr Opin Investig Drugs, V1, P370

[7]

Chenard BL, 1999, CURR PHARM DESIGN, V5, P381

[8]

FISCHER G, 1996, NEUR ANN M NOV 16 21

[9]

Gill R., 1999, CURR OPIN CARDIOVASC, V1, P576

[10] BINDING CHARACTERISTICS OF PRAZOSIN-H-3 TO RAT-BRAIN ALPHA-ADRENERGIC RECEPTORS [J].

GREENGRASS, P ;

BREMNER, R .

EUROPEAN JOURNAL OF PHARMACOLOGY, 1979, 55 (03) :323-326

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