Synthesis and structure-activity relationship of novel benzoxazole derivatives as melatonin receptor agonists.
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.
Sun
Li-Qiang
LQ
Bristol-Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, CT 06492, USA. sunl@bms.com
Chen
Jie
J
Bruce
Marc
M
Deskus
Jeffrey A
JA
Epperson
James R
JR
Takaki
Katherine
K
Johnson
Graham
G
Iben
Lawrence
L
Mahle
Cathy D
CD
Ryan
Elaine
E
Xu
Cen
C
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
D001583:Benzoxazoles; D008024:Ligands; D011956:Receptors, Cell Surface; D044094:Receptors, Melatonin; D008550:Melatonin