New spiro-piperidines as 5-HT2B receptor antagonists.
A functional screening highlighted a series of spiro-piperidines as 5-HT2B receptor antagonists. Preliminary structure-activity relationship has been explored driving to potent antagonists (IC50 = 1 nM) and indicating directions for further explorations.
Bienaymé
Hugues
H
Urogene, Hopital Saint-Louis, 1 Avenue Claude Vellefaux, 75010 Paris, France.
Chêne
Laurent
L
Grisoni
Serge
S
Grondin
Antonio
A
Kaloun
El-Bachir
el-B
Poigny
Stéphane
S
Rahali
Houcine
H
Tam
Eric
E
D020128:Inhibitory Concentration 50; D008024:Ligands; D015394:Molecular Structure; D010880:Piperidines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D044403:Receptor, Serotonin, 5-HT2B / Q000378:metabolism; D058830:Serotonin 5-HT2 Receptor Antagonists; D013329:Structure-Activity Relationship
D008024:Ligands; D010880:Piperidines; D044403:Receptor, Serotonin, 5-HT2B; D058830:Serotonin 5-HT2 Receptor Antagonists