Unidad en Investigación y Desarrollo de Medicamentos, Centro de Investigación en Farmacobiología Aplicada-CIFA, Universidad de Navarra, C/Irunlarrea 1, 31008 Pamplona, Spain.
Molecules. 2012 Jun 25;17(7):7737-57. doi: 10.3390/molecules17077737.
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.
自从人们提出褪黑素可能促进睡眠并使昼夜节律同步的观点以来，许多研究小组都集中精力获得新的褪黑素受体配体，其药效团包括与中央环相连的可变长度的脂肪链、N-烷基酰胺和甲氧基（或生物等排体）。用萘或喹啉环替代褪黑素中的吲哚环会导致具有相似亲和力的化合物。在这种结构近似中，下一步是将喹喔啉环（喹啉和萘环的生物等排体）引入作为未来褪黑素能配体的中心核。
