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Syntheses ofO‐Methylasparvenone‐Derived Serotonin‐Receptor Antagonists

 

作者: Michael Bös,   Heinz Stadler,   Jürgen Wichmann,   François Jenck,   James R. Martin,   Jean‐Luc Moreau,   Andrew J. Sleight,  

 

期刊: Helvetica Chimica Acta  （WILEY Available online 1998）
卷期: Volume 81, issue 3‐4  

页码: 525-538

 

ISSN:0018-019X

 

年代: 1998

 

DOI:10.1002/hlca.19980810306

 

出版商: WILEY‐VCH Verlag GmbH

 

数据来源: WILEY

 

摘要:

AbstractBased onO‐methylasparvenone (1), a N‐free 5HT2Cantagonist with moderate affinity (pKi= 6.7), derivatives bearing dimethylamino (7), (dimethylamino)methyl (17,18,21, and22), and aminomethyl substituents (26) in place of the benzylic OH group of1as well as pyrrolidine‐ (33) and piperidine‐fused derivatives (29,43, and45) were synthesized. In contrast to the lead structure1, these new ligands were activein vivoin the rat. The tricycles33and45display high affinities for the 5HT2Creceptor (

 

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