European Journal of Medicinal Chemistry p. 621 - 631 (2017)
Update date:2022-08-10
Topics:
Landagaray, Elodie
Ettaoussi, Mohamed
Rami, Marouan
Boutin, Jean A.
Caignard, Daniel-Henri
Delagrange, Philippe
Melnyk, Patricia
Berthelot, Pascal
Yous, Sa?d
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 MT2selectivity. Besides, sulphonamide 11b showed the most important MT2selectivity of this series (167 folds) while methyl and ethyl-ureas 11f and 11g represented the most potent melatonergic ligands of this study.
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