NOVEL NONOPIOID NON-ANTIINFLAMMATORY ANALGESICS - 3-(AMINOALKYL) AND 3-[(4-ARYL-1-PIPERAZINYL)ALKYL]OXAZOLO[4,5-B]PYRIDIN-2(3H)-ONES

被引:47
作者
FLOUZAT, C
BRESSON, Y
MATTIO, A
BONNET, J
GUILLAUMET, G
机构
[1] UNIV ORLEANS,CNRS,CHIM BIOORGAN & ANALYT LAB,BP 6759,F-45067 ORLEANS 2,FRANCE
[2] INST RECH SERVIER,F-92150 SURESNES,FRANCE
关键词
D O I
10.1021/jm00056a010
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of 3-(aminoalkyl)- and 3-[(4-aryl-1-piperazinyl)alkyl]oxazolo[4,5-b]pyridin-2(3H)-ones were prepared from their respective oxazolo[4,5-b]pyridin-2(3H)-ones. Several members of this group were found to possess potent analgesic activity in the mouse during a p-phenylquinone writhing induced test. Among them, phenylpiperazine compounds with two-carbon length alkyl chains, 2a and 2b, appeared by high analgesic with little toxicity having neither an antiinflammatory effect nor opioid receptor affinity. The synthesis and structure-affinity relationships for this series are detailed.
引用
收藏
页码:497 / 503
页数:7
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