Discovery of new C3aR ligands. Part 2: Amino-piperidine derivatives

The synthesis and structure–activity relationships against the C3a receptor of a series of substituted aminopiperidine derivatives are reported. DMPK properties and functional activities of selected compounds are described. The compounds obtained are the first non-arginine ligands of C3aR.

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2007-06, Vol.17 (12), p.3262-3265
Hauptverfasser: Denonne, Frédéric, Binet, Sophie, Burton, Maggi, Collart, Philippe, Defays, Sabine, Dipesa, Alan, Eckert, Maria, Giannaras, Alexander, Kumar, Seema, Levine, Beth, Nicolas, Jean-Marie, Pasau, Patrick, Pégurier, Cécile, Preda, Dorin, Van houtvin, Nathalie, Volosov, Andrew, Zou, Dong
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container_end_page 3265
container_issue 12
container_start_page 3262
container_title Bioorganic & medicinal chemistry letters
container_volume 17
creator Denonne, Frédéric
Binet, Sophie
Burton, Maggi
Collart, Philippe
Defays, Sabine
Dipesa, Alan
Eckert, Maria
Giannaras, Alexander
Kumar, Seema
Levine, Beth
Nicolas, Jean-Marie
Pasau, Patrick
Pégurier, Cécile
Preda, Dorin
Van houtvin, Nathalie
Volosov, Andrew
Zou, Dong
description The synthesis and structure–activity relationships against the C3a receptor of a series of substituted aminopiperidine derivatives are reported. DMPK properties and functional activities of selected compounds are described. The compounds obtained are the first non-arginine ligands of C3aR.
doi_str_mv 10.1016/j.bmcl.2007.04.023
format Article
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1464-3405
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source MEDLINE; ScienceDirect Journals (5 years ago - present)
subjects Agonist
Amines - chemistry
Animals
Biological and medical sciences
C3a
Complement Activation - drug effects
Inflammation
Ligands
Medical sciences
Membrane Proteins - metabolism
Mice
Mice, Inbred BALB C
Pharmacology. Drug treatments
Piperidines - chemical synthesis
Piperidines - pharmacology
Protein Binding
Protein-Serine-Threonine Kinases - metabolism
Receptors, Complement - metabolism
Respiratory system
SAR
Structure-Activity Relationship
title Discovery of new C3aR ligands. Part 2: Amino-piperidine derivatives
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