SYNTHESIS AND BIOLOGICAL EVALUATION OF A SERIES OF SUBSTITUTED N-ALKOXYIMIDES AND N-ALKOXYAMIDES AS POTENTIAL ATYPICAL ANTIPSYCHOTIC AGENTS

被引：15

作者：

HRIB, NJ ^{[1
]}

JURCAK, JG ^{[1
]}

HUGER, FP ^{[1
]}

ERRICO, CL ^{[1
]}

DUNN, RW ^{[1
]}

机构：

[1] HOECHST ROUSSEL PHARMACEUT PROPRIETARY LTD,DEPT BIOL RES,SOMERVILLE,NJ 08876

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1991年 / 34卷 / 03期

关键词：

D O I：

10.1021/jm00107a028

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

In a continuing program to discover antipsychotic agents with a reduced propensity toward extrapyramidal side-effects, a series of N-alkoxyimides and -amides was prepared. Evaluation of these compounds in vitro revealed affinities for D2, 5HT2 and 5HT1a receptors. Several members of the series displayed a profile indicative of potential antipsychotic activity in preclinical assays. The most potent compound in these assays, 7, also displayed possible effectiveness for the negative symptoms of schizophrenia. The synthesis of these compounds and details of their structure-activity relationships are described.

引用

页码：1068 / 1072

页数：5

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