Imidazo[1,2-b]pyridazines .19. Syntheses and central nervous system activities of some 6-arylthio(aryloxy and alkylthio)-3-(acetamidomethyl, benzamidomethyl, methoxy and unsubstituted)-2-arylimidazo[1,2-b]pyridazines

被引:2
作者
Barlin, GB [1 ]
Davies, LP [1 ]
Ireland, SJ [1 ]
机构
[1] AUSTRALIAN NATL UNIV,RES SCH BIOL SCI,VISUAL SCI GRP,CANBERRA,ACT 2601,AUSTRALIA
关键词
D O I
10.1071/CH9960443
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
Some 6-arylthio(aryloxy and alkylthio)-3-(acetamidomethyl, benzamidomethyl, methoxy and unsubstituted)-2-arylimidazo [1,2-b]pyridazines have been prepared and examined for their ability to displace [H-3]diazepam from rat brain membranes. The most active compound was 3-acetamidomethyl-2-(3',4'-methylenedioxyphenyl)-6-phenylthioimidazo [1,2-b]pyridazine with IC50 4 . 4 nM. The 3-acylaminomethyl-6-(2- and 3-methoxyphenylthio)-2-phenylimidazo[1,2-b]pyridazines proved less active than their 6-phenylthio analogues, and larger substituents at the 2- and 6-positions markedly decreased binding. Significant differences in binding ability have been observed between 3-acylaminomethyl-2-aryl-6-phenylthioimidazo[1,2-b]pyridazines and the corresponding imidazo[1,2-a] pyridines.
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页码:443 / 449
页数:7
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