SYNTHESIS, BIOLOGICAL IN-VITRO EVALUATION AND STEREOSELECTIVITY OF ONDANSETRON ANALOGS - NOVEL 5-HT2A RECEPTOR ANTAGONISTS

被引：10

作者：

ELZ, S

HEIL, WL

机构：

[1] Institute of Pharmacy, Freie Universität Berlin, Königin-Luise-Strasse 2 + 4

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1995年 / 5卷 / 07期

关键词：

D O I：

10.1016/0960-894X(95)00092-8

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The tetrahydrocarbazolone moiety of the 5-HT3 receptor antagonist ondansetron has been combined with molecular fragments of typical 5-HT2A receptor ligands. Several of the resulting compounds are potent 5-HT2A antagonists. The antipodes of the most potent compound, a N-substituted 4-(4-fluorobenzoyl)piperidine, are analogues of ketanserin which display a high degree of stereoselectivity at 5-HT2A receptors (148:1).

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页码：667 / 672

页数：6

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