IMIDAZO[1,2-B]PYRIDAZINES .10. SYNTHESES AND CENTRAL-NERVOUS-SYSTEM ACTIVITIES OF SOME 3-(ACETAMIDO, BENZAMIDO, SUBSTITUTED BENZAMIDO OR DIMETHYLAMINO)METHYL-2-(PHENYL OR SUBSTITUTED PHENYL)-6-(HALOGENO, ALKYLTHIO, ALKOXY, PHENYLTHIO, PHENOXY, BENZYLTHIO OR BENZYLOXY)IMIDAZO[1,2-B]PYRIDAZINES

被引:22
作者
BARLIN, GB [1 ]
DAVIES, LP [1 ]
IRELAND, SJ [1 ]
NGU, MML [1 ]
ZHANG, JK [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/CH9920731
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
Syntheses of some 3-(acetamido, benzamido, substituted benzamido or dimethylamino)methyl-2-(phenyl or substituted phenyl)-6-(halogeno, alkylthio, alkoxy, phenylthio, phenoxy, benzylthio or benzyloxy)imidazo[1,2-b]pyridazines from the 3-unsubstituted analogues are described. The IC50 values (or percentage displacements) are reported and discussed for the displacement of [H-3]diazepam from rat brain membrane by each of these compounds. The 3-benzamidomethyl compounds were generally the most active; of these, 3-benzamidomethyl-2-(3',4'-methylenedioxyphenyl)-6-methylthioimidazo[1,2-b]pyridazine showed outstanding activity with IC50 2 nM.
引用
收藏
页码:731 / 749
页数:19
相关论文
共 34 条