[PDF][PDF] A synthetic overview of new molecules with 5-HT1A binding affinities

H Pessoa-Mahana, R Araya-Maturana… - Mini Reviews in …, 2003 - researchgate.net
A Synthetic Overview of New Molecules with 5-HT1A Binding Affinities Page 1 77 A Synthetic
Overview of New Molecules with 5-HT1A Binding Affinities Hernán Pessoa-Mahana*1; Ramiro …

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

P Zajdel, G Subra, AJ Bojarski, B Duszyńska… - Bioorganic & medicinal …, 2006 - Elsevier
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 …

2, 5-Disubstituted pyridines: The discovery of a novel series of 5-HT2A ligands

KJ Wilson, MB van Niel, L Cooper, D Bloomfield… - Bioorganic & medicinal …, 2007 - Elsevier
This report describes the effect of replacing the central basic amine present in many known
5-HT2A ligands with an aromatic residue. We targeted the isomeric phenethylpyridines 2 …

Short and efficient syntheses of analogues of WAY-100635: new and potent 5-HT1A receptor antagonists

S Marchais, B Nowicki, H Wikström, LT Brennum… - Bioorganic & medicinal …, 2001 - Elsevier
Simple syntheses of four new and potent analogues of the 5-HT1A receptor ligand, WAY-
100635 are described, namely the 6-(pyridinyl)-bromo-, the 6-(pyridinyl)-fluoro-, the …

First tricyclic oximino derivatives as 5-HT3 ligands

I Baglin, C Daveu, JC Lancelot, R Bureau… - Bioorganic & medicinal …, 2001 - Elsevier
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Synthesis and evaluation of arylpiperazines derivatives of 3, 5-dioxo-(2H, 4H)-1, 2, 4-triazine as 5-HT1AR ligands

JSD Kumar, VJ Majo, J Prabhakaran… - Bioorganic & medicinal …, 2014 - Elsevier
HT 1A R agonist or partial agonists are established drug candidates for psychiatric and
neurological disorders. We have reported the synthesis and evaluation of a series of high …

New N-and O-arylpiperazinylalkyl pyrimidines and 2-methylquinazolines derivatives as 5-HT7 and 5-HT1A receptor ligands: synthesis, structure-activity relationships …

S Intagliata, MN Modica, V Pittalà, L Salerno… - Bioorganic & medicinal …, 2017 - Elsevier
Based on our earlier studies of structure activity relationships on 4-substituted piperazine
derivatives, in this work we synthesized a novel set of long-chain arylpiperazines with the …

Highly potent, non-basic 5-HT6 ligands. Site mutagenesis evidence for a second binding mode at 5-HT6 for antagonism

RN Harris III, RS Stabler, DB Repke, JM Kress… - Bioorganic & medicinal …, 2010 - Elsevier
A series of 5-HT6 ligands derived from (R)-1-(amino) methyl-6-(phenyl) sulfonyltetralin was
prepared that yielded several non-basic analogs having sub-nanomolar affinity. Ligand …

Discovery of Benzamide Analogues as a Novel Class of 5‐HT3 Receptor Agonists

CG Jørgensen, B Frølund, J Kehler… - ChemMedChem, 2011 - Wiley Online Library
A 5‐HT3 receptor agonist based on a benzamide scaffold was identified in a screening of a
small commercial compound library, and an elaborate SAR study originating from this hit …

Rational design in search for 5-phenylhydantoin selective 5-HT7R antagonists. Molecular modeling, synthesis and biological evaluation

K Kucwaj-Brysz, D Warszycki, S Podlewska… - European journal of …, 2016 - Elsevier
A series of novel arylpiperazine 5-(4-fluorophenyl)-5-methylhydantoins with 2-hydroxypropyl
linker (2–15) was synthesized and evaluated on their affinity towards serotonin 5-HT 7 …