Synthesis and structure-activity relationship of novel benzoxazole derivatives as melatonin receptor agonists.
Article Details
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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
Drug Target Property Measurement pH Temperature (°C) Melatonin Melatonin receptor type 1A Ki (nM) 0.4 N/A N/A Details Melatonin Melatonin receptor type 1B Ki (nM) 0.3 N/A N/A Details