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

Bioorganic & Medicinal Chemistry Letters, ISSN: 0960-894X, Vol: 14, Issue: 14, Page: 3799-3802
2004
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Article Description

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.

Bibliographic Details

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

Elsevier BV

Biochemistry, Genetics and Molecular Biology; Pharmacology, Toxicology and Pharmaceutics; Chemistry

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