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

Li-Qiang Sun; Jie Chen; Marc Bruce; Jeffrey A Deskus; James R Epperson; Katherine Takaki; Graham Johnson; Lawrence Iben; Cathy D Mahle; Elaine Ryan; Cen Xu

doi:10.1016/j.bmcl.2004.04.082

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

Bioorg Med Chem Lett. 2004 Jul 16;14(14):3799-802. doi: 10.1016/j.bmcl.2004.04.082.

Authors

Li-Qiang Sun¹, Jie Chen, Marc Bruce, Jeffrey A Deskus, James R Epperson, Katherine Takaki, Graham Johnson, Lawrence Iben, Cathy D Mahle, Elaine Ryan, Cen Xu

Affiliation

¹ Bristol-Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, CT 06492, USA. [email protected]

PMID: 15203165
DOI: 10.1016/j.bmcl.2004.04.082

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.

MeSH terms

Benzoxazoles / chemical synthesis*
Benzoxazoles / pharmacology
Binding Sites
Cell Line
Drug Design
Humans
Ligands
Melatonin / analogs & derivatives
Melatonin / metabolism
Radioligand Assay
Receptors, Cell Surface / drug effects
Receptors, Melatonin / agonists*
Receptors, Melatonin / metabolism
Structure-Activity Relationship

Substances

Benzoxazoles
Ligands
Receptors, Cell Surface
Receptors, Melatonin
Melatonin