New Quinoxaline Derivatives as Potential MT1 and MT2 Receptor Ligands

被引:11
|
作者
Ancizu, Saioa [1 ]
Castrillo, Nerea [1 ]
Perez-Silanes, Silvia [1 ]
Aldana, Ignacio [1 ]
Monge, Antonio [1 ]
Delagrange, Philippe [2 ]
Caignard, Daniel-Henry [2 ]
Galiano, Silvia [1 ]
机构
[1] Univ Navarra, Unidad Invest & Desarrollo Medicamentos, CIFA, Pamplona 31008, Spain
[2] IdRServier, F-78290 Croissy Sur Seine, France
关键词
sleep disorders; melatonin; MT1/MT2; receptors; quinoxalinamide; quinoxalinurea; CONFORMATIONALLY RESTRICTED LIGANDS; MOLECULAR-FIELD ANALYSIS; MELATONIN RECEPTOR; PHARMACOLOGICAL CHARACTERIZATION; HIGH-AFFINITY; NAPHTHALENIC DERIVATIVES; BIOLOGICAL EVALUATION; BINDING-AFFINITY; DESIGN; SERIES;
D O I
10.3390/molecules17077737
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
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.
引用
收藏
页码:7737 / 7757
页数:21
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