title: 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.
authors.affiliation: Bristol-Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, CT 06492, USA. sunl@bms.com
authors.forename: Li-Qiang
authors.initials: LQ
authors.lastname: Sun
authors.forename: Jie
authors.initials: J
authors.lastname: Chen
authors.forename: Marc
authors.initials: M
authors.lastname: Bruce
authors.forename: Jeffrey A
authors.initials: JA
authors.lastname: Deskus
authors.forename: James R
authors.initials: JR
authors.lastname: Epperson
authors.forename: Katherine
authors.initials: K
authors.lastname: Takaki
authors.forename: Graham
authors.initials: G
authors.lastname: Johnson
authors.forename: Lawrence
authors.initials: L
authors.lastname: Iben
authors.forename: Cathy D
authors.initials: CD
authors.lastname: Mahle
authors.forename: Elaine
authors.initials: E
authors.lastname: Ryan
authors.forename: Cen
authors.initials: C
authors.lastname: Xu
mesh_terms: D001583:Benzoxazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D001665:Binding Sites; D002460:Cell Line; D015195:Drug Design; D006801:Humans; D008024:Ligands; D008550:Melatonin / Q000031:analogs & derivatives / Q000378:metabolism; D011869:Radioligand Assay; D011956:Receptors, Cell Surface / Q000187:drug effects; D044094:Receptors, Melatonin / Q000819:agonists* / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D001583:Benzoxazoles; D008024:Ligands; D011956:Receptors, Cell Surface; D044094:Receptors, Melatonin; D008550:Melatonin