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吡唑并[1,5 - a]吡啶并[3,4 - e]嘧啶 - 6 - 酮。II. 合成及体外抗菌活性评价

Pyrazolo[1,5-a]pyrido[3,4-e]pyrimidin-6-ones. II. Synthesis and in vitro antimicrobial evaluation.

作者信息

Bruni F, Selleri S, Costanzo A, Guerrini G, Ciciani G, Costagli C, Sacco C, Donato R

机构信息

Dipartimento di Scienze Farmaceutiche, Università degli Studi di Firenze, Italy.

出版信息

Farmaco. 1997 Oct;52(10):639-43.

PMID:9507678
Abstract

A series of Pyrazolo[1,5-a]pyrido[3,4-e]pyrimidin-6-ones (4a-p) was prepared by a simple synthetic procedure based on the reaction of hydroxylamine or methoxyamine with 2,3-substituted ethyl 7-dimethylaminovinyl pyrazolo[1,5-a]pyrimidin-6-carboxylates (3a-p). The antimicrobial activity of the obtained compounds was evaluated on a series of standard strains of Gram positive, Gram negative bacteria and fungi. None of the tested compounds showed significant activity.

摘要

基于羟胺或甲氧基胺与2,3-取代的乙基7-二甲基氨基乙烯基吡唑并[1,5-a]嘧啶-6-羧酸酯(3a-p)的反应,通过简单的合成方法制备了一系列吡唑并[1,5-a]吡啶并[3,4-e]嘧啶-6-酮(4a-p)。对所得到的化合物在一系列革兰氏阳性、革兰氏阴性细菌和真菌的标准菌株上进行了抗菌活性评估。所测试的化合物均未显示出显著活性。

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