CONFORMATION-ACTIVITY RELATIONSHIP STUDY OF 5-HT3 RECEPTOR ANTAGONISTS AND A DEFINITION OF A MODEL FOR THIS RECEPTOR-SITE

被引:115
作者
HIBERT, MF
HOFFMANN, R
MILLER, RC
CARR, AA
机构
[1] Merrell Dow Research Institute, 67084 Strasbourg Cedex, 16, rue d'Ankara
关键词
D O I
10.1021/jm00168a011
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A conformation-activity relationship study of 5-HT3 receptor antagonists was used to define a pharmacophore and receptor map to qualitatively account for their activity. The design and synthesis of specific keto-amino-indole derivatives that are potent 5-HT3 receptor antagonists gave some support to the model. © 1990, American Chemical Society. All rights reserved.
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页码:1594 / 1600
页数:7
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