Syntheses, pharmacological evaluation and molecular modelling of substituted 6-alkoxyimidazo [1, 2-b] pyridazines as new ligands for the benzodiazepine receptor

PW Harrison, GB Barlin, LP Davies, SJ Ireland…

文献索引：Harrison, P. W.; Barlin, G. B.; Davies, L. P.; Ireland, S. J.; Matyus, P.; Wong, M. G. European Journal of Medicinal Chemistry, 1996 , vol. 31, # 9 p. 651 - 662

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被引用次数: 24

摘要

A series of 2, 3-disubstituted-6-alkoxyimidazo [1, 2-b] pyridazines has been synthesized and evaluated for in vitro affinity for the benzodiazepine receptor (BZR). 3-(Benzamidomethyl or substituted benzamidomethyl)-6-methoxy-2-(3, 4-methylenedioxyphenyl) imidazo [1, 2-b] pyridazines were found to be the most potent BZR ligands (eg, 4a, IC50 7 nM; 4e, IC50 14 nM; 4v, IC50 8 nM). Imidazo [1, 2-b] pyridazines unsubstituted in the 3-position, or ...