TRICYCLIC HETEROAROMATIC SYSTEMS - [1]BENZOPYRANO-PYRAZOL-4-ONES AS BENZODIAZEPINE RECEPTOR LIGANDS

被引:24
作者
COLOTTA, V
CECCHI, L
MELANI, F
FILACCHIONI, G
MARTINI, C
GELLI, S
LUCACCHINI, A
机构
[1] UNIV FLORENCE,DIPARTIMENTO SCI FARMACEUT,VIA GINO CAPPONI 9,I-50121 FLORENCE,ITALY
[2] UNIV PISA,IST POLICATTEDRA DISCIPLINE BIOL,I-56100 PISA,ITALY
关键词
D O I
10.1002/jps.2600800317
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The synthesis of a series of 8-substituted 1,4-dihydro-1-aryl-3-methyl-[1]benzopyrano[3,4-d]pyrazol-4-ones (series 7) and 2,4-dihydro-2-aryl-3-methyl[1]benzopyranol[4,3-c]pyrazol-4-ones (series 8) is reported. Compounds of series 7 and 8 were tested for their ability to displace [H-3]flunitrazepam from bovine brain membranes and for their in vitro biological activity. The results allowed some conclusions to be drawn about the structural requirements of the benzodiazepine recognition site within this class of unusual ligands.
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收藏
页码:276 / 279
页数:4
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