Synthesis and structure-activity relationship of novel benzoxazole derivatives as melatonin receptor agonists.

Article Details

Citation

Sun LQ, Chen J, Bruce M, Deskus JA, Epperson JR, Takaki K, Johnson G, Iben L, Mahle CD, Ryan E, Xu C

Synthesis and structure-activity relationship of novel benzoxazole derivatives as melatonin receptor agonists.

Bioorg Med Chem Lett. 2004 Jul 16;14(14):3799-802.

PubMed ID
15203165 [ View in PubMed
]
Abstract

A series of benzoxazole derivatives was synthesized and evaluated as melatoninergic ligands. The binding affinity of these compounds for human MT(1) and MT(2) receptors was determined using 2-[(125)I]-iodomelatonin as the radioligand. From this series of benzoxazole derivatives, compounds 14 and 17 were identified as melatonin receptor agonists.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
MelatoninMelatonin receptor type 1AKi (nM)0.4N/AN/ADetails
MelatoninMelatonin receptor type 1BKi (nM)0.3N/AN/ADetails