Synthesis of a novel class of non-peptide NK-2 receptor ligand, derived from 1-phenyl-3-pyrrol-1-ylindan-2-carboxamides

被引：30
作者：
Guillon, J
Dallemagne, P
Léger, JM
Sopkova, J
Bovy, PR
Jarry, C
Rault, S
机构：
[1] Univ Caen, UFR Sci Pharmaceut, Ctr Etud & Rech Medicament Normandie, F-14032 Caen, France
[2] Univ Bordeaux 2, UFR Sci Pharmaceut, EA Pharmacochim 2962, F-33076 Bordeaux, France
[3] Synthelabo LERS, F-92500 Rueil Malmaison, France
来源：
BIOORGANIC & MEDICINAL CHEMISTRY | 2002年 / 10卷 / 04期
关键词：
D O I：
10.1016/S0968-0896(01)00360-1
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
A series of trans,trans-1-phenyl-3-pyrrol-1-ylindan-2-carboxamide derivatives has been synthesized in eight steps starting from cinnamic acid or 3.3-diphenylpropionic acid. The trans,trans configuration of these carboxamides has been established by X-ray analysis and by NOE experiments in NMR. These new compounds were evaluated for their potential NK-1, NK-2 and NK-3 receptors binding affinity. The N,N-disubstituted carboxamides bound selectively on NK-2 receptors. (C) 2002 Elsevier Science Ltd. All rights reserved.
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收藏
页码：1043 / 1050
页数：8
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