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Novel difluoroacetamide analogues of agomelatine and melatonin: probing the melatonin receptors for MT1 selectivity?

MedChemComm Pub Date: 2015-06-08 DOI: 10.1039/C5MD00190K

Abstract

Synthesis and pharmacological evaluation of novel agomelatine and melatonin analogues with structures combining the features generating MT₁ selectivity, namely the bulky hydrophobic ether moiety and the difluoroacetamide group, is reported. The dimeric agomelatine analogue linked by a three methylene spacer displayed the best affinity (K_i = 1.2 nM) and selectivity (7-fold) toward MT₁ receptors.

Graphical abstract: Novel difluoroacetamide analogues of agomelatine and melatonin: probing the melatonin receptors for MT1 selectivity

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MedChemComm

Journal Name：MedChemComm

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