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1. Synthesis of a Novel Class of Non-Peptide NK-2 Receptor Ligand, Derived from 1-Phenyl-3-pyrrol-1-ylindan-2-carboxamides

Author

Guillon, Jean, Dallemagne, Patrick, Léger, Jean-Michel, Sopkova, Jana, Bovy, Philippe R., Jarry, Christian, and Rault, Sylvain

Subjects
*AMIDES, *X-ray spectroscopy, *PROPIONIC acid
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. [Copyright &y& Elsevier]

Published
2002
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