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

Darius P. Zlotos; Noura M. Riad; Mai B. Osman; Bala R. Dodda; Paula A. Witt-Enderby

doi:10.1039/C5MD00190K

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

Darius P. Zlotos,*^a Noura M. Riad,^a Mai B. Osman,^a Bala R. Dodda^b and Paula A. Witt-Enderby^b

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* Corresponding authors

^a Department of Pharmaceutical Chemistry, The German University in Cairo, New Cairo City, 11835 Cairo, Egypt
E-mail: darius.zlotos@guc.edu.eg
Fax: +20 2 2758 1041
Tel: +20 2 2758 1041

^b Division of Pharmaceutical Sciences, School of Pharmacy, Duquesne University, 421 Mellon Hall, Pittsburgh, PA 15282, USA

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.

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Article information

DOI: https://doi.org/10.1039/C5MD00190K
Article type: Concise Article
Submitted: 30 Apr 2015
Accepted: 08 Jun 2015
First published: 08 Jun 2015

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Med. Chem. Commun., 2015,6, 1340-1344

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

D. P. Zlotos, N. M. Riad, M. B. Osman, B. R. Dodda and P. A. Witt-Enderby, Med. Chem. Commun., 2015, 6, 1340 DOI: 10.1039/C5MD00190K

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