O. Diouf, P. Carato, I. Lesieur
1999
Citations
0
Influential Citations
5
Citations
Quality indicators
Journal
European Journal of Medicinal Chemistry
Abstract
Abstract A series of novel 4-(4-fluorobenzoyl)piperidine derivatives with benzothiazolin-2-one as a pivotal template was designed, synthesised and evaluated on a battery of receptors, including serotonin 5-HT 1A , 5-HT 2A and 5-HT 2C , dopamine D 2 and adrenergic α 1 receptors. The 4-(4-fluorobenzoyl)piperidine moiety is known as one of the most potent pharmacophores for the 5-HT 2A receptor. All compounds displayed high affinities for the central 5-HT 2A receptors (1 to 10 nM) combined with high to moderate 5-HT 1A (1 to 800 nM) and D 2 (5 to 1000 nM) affinities. Such a pharmacological profile could lead to new atypical antipsychotics.