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

2008; Elsevier BV; Volume: 16; Issue: 9 Linguagem: Inglês

10.1016/j.bmc.2008.03.036

1464-3391

Mohamed Ettaoussi, Basile Pérès, Frédérique Klupsch, Philippe Delagrange, Jean A. Boutin, Pierre Renard, Daniel-H. Caignard, Philippe Chavatte, Pascal Berthelot, Daniel Lesieur, Saı̈d Yous,

Neurobiology and Insect Physiology Research

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.