IMIDAZO[1,2-B]PYRIDAZINES .12. SYNTHESES AND CENTRAL-NERVOUS-SYSTEM ACTIVITIES OF SOME SUBSTITUTED IMIDAZO[1,2-B]PYRIDAZINES AND RELATED IMIDAZO[1,2-A]PYRIDINES, IMIDAZO[1,2-A]PYRIMIDINES AND IMIDAZO[1,2-A]PYRAZINES

被引:20
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/CH9920877
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
Syntheses are reported for some 6-chloro(alkoxy, alkylthio and phenylthio)-3-benzamidomethyl-(acetamidomethyl and methoxy)-2-arylimidazo[1,2-a]pyridines and some corresponding imidazo[1,2-b]pyridazines, imidazo[1,2-a]pyrimidines and imidazo[1,2-a]pyrazines. IC50 values (or percentage displacement) are reported and discussed for the displacement of [H-3]diazepam from rat brain membrane by each of these compounds. The imidazo[1,2-a]pyridines were generally slightly less potent than the imidazo[1,2-b]pyridazines but considerably more potent than the corresponding imidazo[1,2-a]pyrimidines or imidazo[1,2-a]pyrazines. Substitution of a 2-aryl group by a 2-alkyl group in imidazo[1,2-b]pyridazines led to a significant loss of activity.
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收藏
页码:877 / 888
页数:12
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