A series of phenoxyalkyl and phenylthioalkyl amides were prepared as melatoninergic ligands. Modulation of affinity of the newly synthesized compound by applying SARs around the terminal amide moiety, the alkyl chain, and the methoxy group on the aromatic ring provides compounds with nanomolar affinity for both melatonin receptor subtypes. Affinity towards MT1 and MT2 receptors were modulated also exploiting chirality. The investigation of intrinsic activity revealed that all the tested compounds behave as full or partial agonists.
Design, synthesis, and pharmacological effects of structurally simple ligands for MT1 and MT2 melatonin receptors / A. Carocci, A. Catalano, A. Lovece, G. Lentini, A. Duranti, V. Lucini, M. Pannacci, F. Scaglione, C. Franchini. - In: BIOORGANIC & MEDICINAL CHEMISTRY. - ISSN 0968-0896. - 18:17(2010), pp. 6496-6511.
|Titolo:||Design, synthesis, and pharmacological effects of structurally simple ligands for MT1 and MT2 melatonin receptors|
SCAGLIONE, FRANCESCO (Penultimo)
|Parole Chiave:||Bioisosteres; Melatonin; MT1 and MT2 receptors; Phenoxyalkyl amides|
|Settore Scientifico Disciplinare:||Settore BIO/14 - Farmacologia|
|Data di pubblicazione:||2010|
|Digital Object Identifier (DOI):||http://dx.doi.org/10.1016/j.bmc.2010.06.100|
|Appare nelle tipologie:||01 - Articolo su periodico|