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

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

Bioorg Med Chem Lett. 2006 Jul 1;16(13):3406-10. doi: 10.1016/j.bmcl.2006.04.035. Epub 2006 May 3.

Authors

Paweł Zajdel¹, Gilles Subra, Andrzej J Bojarski, Beata Duszyńska, Maciej Pawłowski, Jean Martinez

Affiliation

¹ Laboratoire des Aminoacides, Peptides et Protéines, LAPP, UMR 5810, Faculté de Pharmacie, Université Montpellier I et II, 15 Avenue Charles Flahault, 34060 Montpellier, France. mfzajdel@cyf-kr.edu.pl

PMID: 16677812
DOI: 10.1016/j.bmcl.2006.04.035

Abstract

A library consisting of 60 arylpiperazines modified with N-acylated amino acids was prepared on BAL linker SynPhasetrade mark Lanterns and evaluated in vitro for 5-HT(1A) 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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Acetylation
Amino Acids / chemical synthesis*
Amino Acids / chemistry
Amino Acids / pharmacology*
Combinatorial Chemistry Techniques
Drug Evaluation, Preclinical
Ligands
Molecular Structure
Piperazines / chemical synthesis*
Piperazines / chemistry
Piperazines / pharmacology*
Receptor, Serotonin, 5-HT1A / drug effects*
Stereoisomerism
Structure-Activity Relationship

Substances

Amino Acids
Ligands
Piperazines
Receptor, Serotonin, 5-HT1A