Arylpiperazines with N-acylated amino acids as 5-HT1A receptor ligands

Paweł Zajdel; Gilles Subra; Andrzej J. Bojarski; Beata Duszyńska; Maciej Pawłowski; Jean Martinez

doi:10.1016/j.bmcl.2006.04.035

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Arylpiperazines with N-acylated amino acids as 5-HT1A receptor ligands

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Arylpiperazines with N-acylated amino acids as 5-HT1A receptor ligands

Paweł Zajdel, Gilles Subra, Andrzej J. Bojarski, Beata Duszyńska, Maciej Pawłowski et Jean Martinez

Bioorganic & medicinal chemistry letters, Vol.16(13), pp.3406-3410

01/07/2006

DOI: https://doi.org/10.1016/j.bmcl.2006.04.035

PMID: 16677812

Résumé

5-HT1A receptor ligands

BAL linker

Fujita–Ban analysis

Long-chain arylpiperazines

Pyroglutamates

Solid-phase synthesis

Succinimides

A library consisting of 60 arylpiperazines modified with N-acylated amino acids was prepared on BAL linker SynPhase™ Lanterns and evaluated in vitro for 5-HT1A receptor affinity. Biological screening, followed by a simple Fujita–Ban analysis, enabled the description of structure–activity relationships and allowed the selection of some potent, high-affinity ligands for in vivo pharmacological investigations.

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Titre: Arylpiperazines with N-acylated amino acids as 5-HT1A receptor ligands
Créateurs - sans rôle: Paweł Zajdel - Laboratoire des Aminoacides, Peptides et Protéines (LAPP), UMR 5810, Faculté de Pharmacie, Université Montpellier I et II, 15 Avenue Charles Flahault, 34060 Montpellier, France
Gilles Subra - Laboratoire des Aminoacides, Peptides et Protéines (LAPP), UMR 5810, Faculté de Pharmacie, Université Montpellier I et II, 15 Avenue Charles Flahault, 34060 Montpellier, France
Andrzej J. Bojarski - Polish Academy of Sciences
Beata Duszyńska - Polish Academy of Sciences
Maciej Pawłowski - Department of Medicinal Chemistry, Jagiellonian University Medical College, 9 Medyczna Street, 30-688 Kraków, Poland
Jean Martinez - Laboratoire des Aminoacides, Peptides et Protéines (LAPP), UMR 5810, Faculté de Pharmacie, Université Montpellier I et II, 15 Avenue Charles Flahault, 34060 Montpellier, France
Détails de publication: Bioorganic & medicinal chemistry letters, Vol.16(13), pp.3406-3410
Éditeur: Elsevier Ltd
Nombre de pages: 5
Identifiants: 99163328209311
Unité académique: Institut des Biomolécules Max Mousseron - IBMM
Langue: English
Type de ressource: Journal article