Design and synthesis of benzofuranic derivatives as new ligands at the melatonin-binding site MT3.

Article Details

Citation

Copy to clipboard

Ettaoussi M, Peres B, Klupsch F, Delagrange P, Boutin JA, Renard P, Caignard DH, Chavatte P, Berthelot P, Lesieur D, Yous S

Design and synthesis of benzofuranic derivatives as new ligands at the melatonin-binding site MT3.

Bioorg Med Chem. 2008 May 1;16(9):4954-62. doi: 10.1016/j.bmc.2008.03.036. Epub 2008 Mar 17.

PubMed ID

18372181 [ View in PubMed

]

Abstract

Benzofuranic analogues of MCA-NAT (5-methoxycarbonylamino-N-acetyltryptamine) have been synthesized and evaluated as melatonin receptor ligands. Introduction of a methoxycarbonylamino substituent in the C-5 position of the benzofurane nucleus obtains MT(3) selective ligands. This selectivity can be modulated with suitable variations of the C-5 position and the acyl group on the C-3 side chain.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Melatonin	Melatonin receptor type 1A	IC 50 (nM)	0.2	N/A	N/A	Details
Melatonin	Melatonin receptor type 1B	IC 50 (nM)	0.53	N/A	N/A	Details