New Quinoxaline Derivatives as Potential MT1 and MT2 Receptor Ligands

Molecules

Saioa Ancizu¹  Nerea Castrillo¹  Silvia Pérez-Silanes¹  Ignacio Aldana¹  Antonio Monge¹  Philippe Delagrange¹  Daniel-Henry Caignard¹ 

[1] ¹Unidad en Investigación y Desarrollo de Medicamentos, Centro de Investigación en Farmacobiología Aplicada (CIFA), Universidad de Navarra, C/Irunlarrea, 1, 31008 Pamplona, Spain ²IdRServier, 125 Chemin de ronde, 78290 Croissy-sur-Seine, France

关键词: sleep disorders;    melatonin;    MT₁/MT₂ receptors;    quinoxalinamide;    quinoxalinurea;   

DOI  :  10.3390/molecules17077737

来源: mdpi

【 摘 要 】

Ever since the idea arose that melatonin might promote sleep and resynchronize circadian rhythms, many research groups have centered their efforts on obtaining new melatonin receptor ligands whose pharmacophores include an aliphatic chain of variable length united to an N-alkylamide and a methoxy group (or a bioisostere), linked to a central ring. Substitution of the indole ring found in melatonin with a naphthalene or quinoline ring leads to compounds of similar affinity. The next step in this structural approximation is to introduce a quinoxaline ring (a bioisostere of the quinoline and naphthalene rings) as the central nucleus of future melatoninergic ligands.

【 授权许可】

CC BY   
This is an open access article distributed under the Creative Commons Attribution License (CC BY) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.