CONFORMATIONALLY RESTRICTED THIAZOLE DERIVATIVES AS NOVEL CLASS OF 5-HT3 RECEPTOR LIGANDS

被引:0
|
作者
PERRONE, R [1 ]
BERARDI, F [1 ]
COLABUFO, NA [1 ]
TORTORELLA, V [1 ]
LOGRANO, MD [1 ]
DANIELE, E [1 ]
GOVONI, S [1 ]
机构
[1] DIPARTIMENTO FARMACOBIOL,I-70126 BARI,ITALY
来源
FARMACO | 1995年 / 50卷 / 02期
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中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
A new series of tricyclic derivatives of 2-methyl-naphtho[1,2-d] thiazole were synthesized in order to investigate the effects of the conformational restriction of bicyclic thiazole derivatives previously reported on the 5-HT3 receptor affinity. The basic moiety in these compounds is represented by the terminal nitrogen of N-methyl-piperazine or N-methyl-piperidine ring linked at 2-methyl. All the tricyclic derivatives have a significant 5-HT3 receptor binding affinity and the terminal piperazine ring is more suitable than piperidine one.
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页码:77 / 82
页数:6
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