Synthesis and pharmacological assessment of derivatives of isoxazolo[4,5-d]pyrimidine

Synthesis and pharmacological assessment of derivatives of isoxazolo[4,5-d]pyrimidine
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DOI:
10.1016/j.bmc.2003.10.004
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发表时间:
2004-01-02
影响因子:
3.5
通讯作者:
Nowakowska, E
Nowakowska, E
中科院分区:
医学3区
文献类型:
--
作者:
Wagner, E;Becan, L;Nowakowska, E

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以4-氨基-3-氧代异恶唑烷-5-甲酰胺为原料,合成了一系列新的5-烷基和5-芳基异恶唑并[4,5-d]嘧啶酮(5a-g,6-8)。一些异恶唑并[4,5-d]嘧啶的芳基衍生物与地西泮进行了对比试验。化合物5 b-d和7显示出有趣的抗焦虑活性。(匕首)(C)2003 Elsevier Ltd.保留所有权利。
A series of new 5-alkyl and 5-arylisoxazolo[4,5-d]pyrimidinones (5a-g, 6-8) were prepared from 4-amino-3-oxo-isoxazolidine-5-carboxylic acid amide. Some of the aryl derivatives of isoxazolo[4,5-d]pyrimidine were tested pharmacologically in comparison with Diazepam. Compounds 5b-d and 7 demonstrated interesting anxiolytic activity.(dagger) (C) 2003 Elsevier Ltd. All rights reserved.