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New Quinoxaline Derivatives as Potential MT1 and MT2 Receptor Ligands
Unidad en Investigación y Desarrollo de Medicamentos, Centro de Investigación en Farmacobiología Aplicada (CIFA), Universidad de Navarra, C/Irunlarrea, 1, 31008 Pamplona, Spain
IdRServier, 125 Chemin de ronde, 78290 Croissy-sur-Seine, France
* Author to whom correspondence should be addressed.
Received: 17 April 2012; in revised form: 14 June 2012 / Accepted: 18 June 2012 / Published: 25 June 2012
Abstract: 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.
Keywords: sleep disorders; melatonin; MT1/MT2 receptors; quinoxalinamide; quinoxalinurea
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Ancizu, S.; Castrillo, N.; Pérez-Silanes, S.; Aldana, I.; Monge, A.; Delagrange, P.; Caignard, D.-H.; Galiano, S. New Quinoxaline Derivatives as Potential MT1 and MT2 Receptor Ligands. Molecules 2012, 17, 7737-7757.
Ancizu S, Castrillo N, Pérez-Silanes S, Aldana I, Monge A, Delagrange P, Caignard D-H, Galiano S. New Quinoxaline Derivatives as Potential MT1 and MT2 Receptor Ligands. Molecules. 2012; 17(7):7737-7757.
Ancizu, Saioa; Castrillo, Nerea; Pérez-Silanes, Silvia; Aldana, Ignacio; Monge, Antonio; Delagrange, Philippe; Caignard, Daniel-Henry; Galiano, Silvia. 2012. "New Quinoxaline Derivatives as Potential MT1 and MT2 Receptor Ligands." Molecules 17, no. 7: 7737-7757.