Synthesis of a novel class of non-peptide NK-2 receptor ligand, derived from 1-phenyl-3-pyrrol-1-ylindan-2-carboxamides |
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Authors: | Guillon Jean Dallemagne Patrick Léger Jean-Michel Sopkova Jana Bovy Philippe R Jarry Christian Rault Sylvain |
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Institution: | EA 2962-Pharmacochimie, UFR des Sciences Pharmaceutiques, Université Victor Segalen Bordeaux 2, 146, rue Léo Saignat, 33076 Cedex, Bordeaux, France. |
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Abstract: | 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. |
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