SYNTHESIS AND EVALUATION OF A SERIES OF ARYL[E]FUSED PYRAZOLO[4,3-C]PYRIDINES WITH POTENTIAL ANXIOLYTIC ACTIVITY

被引：30

作者：

FORBES, IT ^{[1
]}

JOHNSON, CN ^{[1
]}

JONES, GE ^{[1
]}

LOUDON, J ^{[1
]}

NICHOLASS, JM ^{[1
]}

THOMPSON, M ^{[1
]}

UPTON, N ^{[1
]}

机构：

[1] BEECHAM PHARMACEUT,MRC,HARLOW,ESSEX,ENGLAND

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1990年 / 33卷 / 09期

关键词：

D O I：

10.1021/jm00171a046

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of pyrazolo[4,3-c]pyridines has been synthesized and evaluated as potential anxiolytic agents. Selected compounds from this series show a pharmacological profile of action different from that of diazepam. A number of the compounds possess higher affinity for central benzodiazepine receptors than diazepam, yet show less anticonvulsant activity and are less sedative. The structure-activity relationships of these potential anxiolytic agents are discussed. © 1990, American Chemical Society. All rights reserved.

引用

页码：2640 / 2645

页数：6

共 22 条

[1] AN ANTIMALARIAL ALKALOID FROM HYDRANGEA .19. THIOPHENE ISOSTERS
BAKER, BR
JOSEPH, JP
SCHAUB, RE
MCEVOY, FJ
WILLIAMS, JH
[J]. JOURNAL OF ORGANIC CHEMISTRY, 1953, 18 (02) : 138 - 152
[2] BARKER J, 1978, J CHEM RES M, P4701
[3] CGS-9896 - A NONBENZODIAZEPINE, NONSEDATING POTENTIAL ANXIOLYTIC
BENNETT, DA
PETRACK, B
[J]. DRUG DEVELOPMENT RESEARCH, 1984, 4 (01) : 75 - 82
[4] LIGANDS FOR BENZODIAZEPINE RECEPTORS WITH POSITIVE AND NEGATIVE EFFICACY
BRAESTRUP, C
HONORE, T
NIELSEN, M
PETERSEN, EN
JENSEN, LH
[J]. BIOCHEMICAL PHARMACOLOGY, 1984, 33 (06) : 859 - 862
[5] COURVOISIER SIMONE, 1956, JOUR CLIN AND EXPTL PSYCHOPATH AND QUART REV PSYCHIATRY AND NEUROL, V17, P25
[6] Everett GM, 1944, J PHARMACOL EXP THER, V81, P402
[7] FORBES IT, Patent No. 126970
[8] Fryer R.I., 1983, BENZODIAZEPINES MOL, P7
[9] THE EFFECTS OF MEPROBAMATE, BARBITURATES, D-AMPHETAMINE AND PROMAZINE ON EXPERIMENTALLY INDUCED CONFLICT IN THE RAT
GELLER, I
SEIFTER, J
[J]. PSYCHOPHARMACOLOGIA, 1960, 1 (06): : 482 - 492
[10] MECHANISM OF DIECKMANN-REACTION OF METHYL-3-(METHOXY-CARBONYLMETHYLTHIO)-PROPIONATE
HROMATKA, O
BINDER, D
EICHINGE.K
[J]. MONATSHEFTE FUR CHEMIE, 1973, 104 (06): : 1520 - 1525

← 1 2 3 →