New quinolinic derivatives as melatonergic ligands: Synthesis and pharmacological evaluation

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• 作者：Elodie Landagaray^a ; ¹ ; Mohamed Ettaoussi^a ; ¹ ; ^{m.ettaoussi@yahoo.fr} ; Marouan Rami^a ; Jean A. Boutin^b ; Daniel-Henri Caignard^c ; Philippe Delagrange^c ; Patricia Melnyk^a ; ^d ; Pascal Berthelot^a ; ^d ; Saï ; d Yous^a ; ^d ; ^{said.yous@univ-lille2.fr}
• 关键词：Melatonin ; Quinoline derivatives ; MT1 ; MT2-Selectivity ; Agonist
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：15 February 2017
• 年：2017
• 卷：127
• 期：Complete
• 页码：621-631
• 全文大小：690 K
• 卷排序：127

文摘

New quinolines were prepared as melatoninergic ligands. Synthesized derivatives showed good binding affinities at both MT1 and MT2. Sulphonamide 11b showed an important MT2 selectivity of about 167. Methylurea 11f and ethylurea 11g represented the most potent of this series.