Structure-activity studies of aryl-spaced decahydroisoquinoline-3-carboxylic acid AMPA receptor antagonists

被引：23

作者：

Bleisch, TJ

Ornstein, PL

Allen, NK

Wright, RA

Lodge, D

Schoepp, DD

机构：

[1] LILLY CORP CTR,LILLY RES LABS,INDIANAPOLIS,IN 46285

[2] LILLY RES CTR LTD,WINDLESHAM GU20 6PH,SURREY,ENGLAND

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1997年 / 7卷 / 09期

关键词：

D O I：

10.1016/S0960-894X(97)00185-6

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We report the synthesis and structure activity studies of a series of decahydroisoquinoline AMPA antagonists where the distal acid is joined to the bicyclic ring nucleus with a spacer that contains an aromatic ring. These phenyl and thienyl substituted compounds are characterized as relatively potent AMPA antagoinsts. (C) 1997 Elsevier Science Ltd.

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页码：1161 / 1166

页数：6

相关论文

共 19 条

[1] Evidence for prolonged release of excitatory amino acids in severe human head trauma - Relationship to clinical events [J].

Bullock, R ;

Zauner, A ;

Myseros, JS ;

Marmarou, A ;

Woodward, JJ ;

Young, HF .

NEUROPROTECTIVE AGENTS: CLINICAL AND EXPERIMENTAL ASPECTS, 1995, 765 :290-297

[2]

DOBLE A, 1995, THERAPIE, V50, P319

[3] New developments in the molecular pharmacology of alpha-amino-3-hydroxy-5-methyl-4-isoxazole propionate and kainate receptors [J].

Fletcher, EJ ;

Lodge, D .

PHARMACOLOGY & THERAPEUTICS, 1996, 70 (01) :65-89

[4]

GILL R, 1994, CEREBROVAS BRAIN MET, V6, P225

[5]

GREENAMYRE JT, 1993, CEREBROVAS BRAIN MET, V5, P61

[6] Bioenergetics and glutamate excitotoxicity [J].

Greene, JG ;

Greenamyre, JT .

PROGRESS IN NEUROBIOLOGY, 1996, 48 (06) :613-+

[7] QUANTITATIVE STUDIES ON SOME ANTAGONISTS OF N-METHYL D-ASPARTATE IN SLICES OF RAT CEREBRAL-CORTEX [J].

HARRISON, NL ;

SIMMONDS, MA .

BRITISH JOURNAL OF PHARMACOLOGY, 1985, 84 (02) :381-391

[8] CHARACTERIZATION OF THE BINDING OF [H-3] CGS-19755 - A NOVEL N-METHYL-D-ASPARTATE ANTAGONIST WITH NANOMOLAR AFFINITY IN RAT-BRAIN [J].

MURPHY, DE ;

HUTCHISON, AJ ;

HURT, SD ;

WILLIAMS, M ;

SILLS, MA .

BRITISH JOURNAL OF PHARMACOLOGY, 1988, 95 (03) :932-938

[9]

NIELSEN EO, 1986, EUR J MED CHEM, V21, P433

[10] Structure-activity studies of 6-(tetrazolylalkyl)-substituted decahydroisoquinoline-3-carboxylic acid AMPA receptor antagonists .1. Effects of stereochemistry, chain length, and chain substitution [J].

Ornstein, PL ;

Arnold, MB ;

Allen, NK ;

Bleisch, T ;

Borromeo, PS ;

Lugar, CW ;

Leander, JD ;

Lodge, D ;

Schoepp, DD .

JOURNAL OF MEDICINAL CHEMISTRY, 1996, 39 (11) :2219-2231