Influence of Lipophilicity on the Biological Activity of Cyclic Pseudopeptide NK-2 Receptor Antagonists

A series of cyclic pseudopeptides of the formula cyclo(Leu psi[CH2NH]Xaa-Gln-Trp-Phe-beta Ala), where Xaa represents the residue of an alpha-amino acid, has been synthesized in order to establish the role of the Xaa side chain for tachykinin NK-2 receptor antagonist activity. Syntheses have been car...

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Veröffentlicht in:	Journal of medicinal chemistry 1994-10, Vol.37 (21), p.3630-3638
Hauptverfasser:	Quartara, Laura, Fabbri, Gaetano, Ricci, Renzo, Patacchini, Riccardo, Pestellini, Vittorio, Maggi, Carlo Alberto, Pavone, Vincenzo, Giachetti, Antonio, Arcamone, Federico
Format:	Artikel
Sprache:	eng
Schlagworte:	Alkylation Amino Acid Sequence Animals Biological Assay Chemistry Chromatography, High Pressure Liquid Cricetinae Cyclization Exact sciences and technology Lipid Metabolism Male Mesocricetus Molecular Sequence Data Organic chemistry Peptides Peptides - chemistry Peptides - pharmacology Peptides, Cyclic - chemical synthesis Peptides, Cyclic - pharmacology Preparations and properties Pulmonary Artery - metabolism Rabbits Receptors, Neurokinin-2 - antagonists & inhibitors Structure-Activity Relationship Trachea - metabolism
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