New insights into homopiperazine-based 5-HT1A/5-HT7R ligands: synthesis and biological evaluation.
The synthesis of new N-homopiperazinyl-based ligands is reported. Various structural modifications along with the corresponding biological activities on 5-HT(1A)/5-HT(7) receptors give further insights into this class of serotoninergic ligands. Among the tested central heterocyles, the 7-azaindole gave the best results on the above-mentioned receptors.
Badarau
Eduard
E
ICOA/University of Orléans, Orléans, France.
Putey
Aurélien
A
Suzenet
Franck
F
Joseph
Benoit
B
Bojarski
Andrzej
A
Finaru
Adriana
A
Guillaumet
Gérald
G
D015195:Drug Design; D006801:Humans; D007211:Indoles; D008024:Ligands; D000077489:Piperazine; D010879:Piperazines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D011485:Protein Binding; D011869:Radioligand Assay; D044282:Receptor, Serotonin, 5-HT1A; D011985:Receptors, Serotonin; D017366:Serotonin Receptor Agonists / Q000138:chemical synthesis / Q000737:chemistry*; D013329:Structure-Activity Relationship
C023422:7-azaindole dimer; D007211:Indoles; D008024:Ligands; D010879:Piperazines; D011985:Receptors, Serotonin; D017366:Serotonin Receptor Agonists; C104425:serotonin 7 receptor; D044282:Receptor, Serotonin, 5-HT1A; D000077489:Piperazine