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

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.