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

来源：

AUSTRALIAN JOURNAL OF CHEMISTRY | 1992年 / 45卷 / 04期

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

页码：731 / 749

页数：19

共 34 条

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