(PLUS-OR-MINUS)11-AMINO-2,6-DIMETHYL-1,2,3,4-TETRAHYDRO-6H-QUININDOLIN-1-ONE, A NOVEL GABA(A) MODULATOR WITH POTENTIAL ANXIOLYTIC ACTIVITY

被引:9
作者
BLACKBURN, TP [1 ]
BOLTON, D [1 ]
FORBES, IT [1 ]
JOHNSON, CN [1 ]
MARTIN, RT [1 ]
THOMAS, DR [1 ]
THOMPSON, M [1 ]
UPTON, N [1 ]
机构
[1] SMITHKLINE BEECHAM PHARMACEUT,HARLOW CM19 5AD,ESSEX,ENGLAND
关键词
D O I
10.1016/S0960-894X(01)80129-3
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Ketone isosteres have been investigated in a series of pyrido[2,3-b]indoles (alpha-carbolines). The incorporation of ring fusion into alpha-carbolines to produce the rigid quinindoline nucleus provides a GABA(A) modulator with both increased potency and a longer duration of action.
引用
收藏
页码:279 / 284
页数:6
相关论文
共 11 条
[1]  
BOLTON D, IN PRESS BIOMED CHEM
[2]   SYNTHESES OF FUNCTIONALIZED PYRIDO[2,3-B]INDOLES [J].
FORBES, IT ;
JOHNSON, CN ;
THOMPSON, M .
JOURNAL OF THE CHEMICAL SOCIETY-PERKIN TRANSACTIONS 1, 1992, (02) :275-281
[3]  
FORBES LT, Patent No. 5079246
[4]   THE EFFECTS OF MEPROBAMATE, BARBITURATES, D-AMPHETAMINE AND PROMAZINE ON EXPERIMENTALLY INDUCED CONFLICT IN THE RAT [J].
GELLER, I ;
SEIFTER, J .
PSYCHOPHARMACOLOGIA, 1960, 1 (06) :482-492
[5]  
HANNIN I, 1977, ANIMAL MODELS PSYCHI
[6]  
HANSCH C, 1990, COMPREHENSIVE MED CH, V4, P402
[7]   PARTITION COEFFICIENTS AND THEIR USES [J].
LEO, A ;
HANSCH, C ;
ELKINS, D .
CHEMICAL REVIEWS, 1971, 71 (06) :525-+
[8]  
MAKSAY G, 1986, MOL PHARMACOL, V30, P321
[9]   FACILITATION OF BENZODIAZEPINE BINDING BY SODIUM-CHLORIDE AND GABA [J].
MARTIN, IL ;
CANDY, JM .
NEUROPHARMACOLOGY, 1978, 17 (11) :993-998
[10]  
TRIFILETTI RR, 1984, MOL PHARMACOL, V26, P470