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Eur J Med Chem. 2017 Feb 15;127:621-631. doi: 10.1016/j.ejmech.2016.12.013. Epub 2017 Jan 3.

New quinolinic derivatives as melatonergic ligands: Synthesis and pharmacological evaluation.

Author information

1
Université de Lille, EA4481 - GRIIOT, F-59000 Lille, France.
2
Université de Lille, EA4481 - GRIIOT, F-59000 Lille, France. Electronic address: m.ettaoussi@yahoo.fr.
3
Biotechnologies, Pharmacologie Moléculaire et Cellulaire, Institut de Recherches Servier, 78290 Croissy-sur-Seine, France.
4
Unité de Recherche Chimie Neurosciences, Institut de Recherches Servier, 78290 Croissy-sur-Seine, France.
5
Université de Lille, EA4481 - GRIIOT, F-59000 Lille, France; Univ. Lille, Inserm, CHU Lille, UMRS-1172 - JPArc - Centre de Recherches Jean-Pierre Aubert Neurosciences et Cancer, F-59000 Lille, France.
6
Université de Lille, EA4481 - GRIIOT, F-59000 Lille, France; Univ. Lille, Inserm, CHU Lille, UMRS-1172 - JPArc - Centre de Recherches Jean-Pierre Aubert Neurosciences et Cancer, F-59000 Lille, France. Electronic address: said.yous@univ-lille2.fr.

Abstract

New series of melatonergic ligands issued from two methoxy-quinolinic scaffolds (2-MQ and 3-MQ), were designed and synthesized. Herein we report the synthetic scheme and pharmacological results of the new prepared compounds. Investigation of compound 11a, the strict 2-MQ analogue, revealed the promising potential of this series. Therefore, pharmacomodulation of the acetamide function of 11a has led to compounds with different pharmacological profiles and the emergence of an MT2 selectivity. Besides, sulphonamide 11b showed the most important MT2 selectivity of this series (167 folds) while methyl and ethyl-ureas 11f and 11g represented the most potent melatonergic ligands of this study.

KEYWORDS:

Agonist; MT(1); MT(2)-Selectivity; Melatonin; Quinoline derivatives

PMID:
28131094
DOI:
10.1016/j.ejmech.2016.12.013
[Indexed for MEDLINE]

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