IMIDAZO[1,2-B]PYRIDAZINES .17. SYNTHESIS AND CENTRAL-NERVOUS-SYSTEM ACTIVITY OF SOME 6-(ALKYLTHIO AND CHLORO)-3-(METHOXY, UNSUBSTITUTED AND BENZAMIDOMETHYL)-2-ARYLIMIDAZO[1,2-B]PYRIDAZINES CONTAINING METHOXY, METHYLENEDIOXY AND METHYL SUBSTITUENTS

被引:16
作者
BARLIN, GB [1 ]
DAVIES, LP [1 ]
DAVIS, RA [1 ]
HARRISON, PW [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/CH9942001
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
Syntheses are reported for 6-(methylthio, ethylthio, propylthio, substituted benzylthio and chloro)-3-(methoxy, unsubstituted and benzamidomethyl)-2-arylimidazo[1,2-b]pyridazines containing methoxy, methylenedioxy and methyl groups attached to phenyl substituents. In tests of the ability of these compounds to displace [H-3]diazepam from rat brain membranes, 3-methoxy-6(3',4'-methylenedioxybenzylthio)-2-(3'',4'' -methylenedioxyphenyl)imidazo[1,2-b]pyridazine (IC50 1 nM) bound most strongly; methylenedioxy groups were beneficial to activity whereas polymethoxy or dimethyl substituents were generally detrimental.
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页码:2001 / 2012
页数:12
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