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一些具有潜在抗真菌活性的新型4,6-二取代-1,2,4-三嗪-3,5(2H)二酮及相关化合物的合成。

Synthesis of some new 4,6-disubstituted-1,2,4-triazin-3,5(2H) diones and related compounds of potential antifungal activity.

作者信息

Abdel-Rahman R M, Seada M, el-Gendy Z, Islam I E, Mahmoud M B

机构信息

Chemistry Department, Faculty of Education, Ain Shams University, Roxy, Cairo, Egypt.

出版信息

Farmaco. 1993 Mar;48(3):407-16.

PMID:8323672
Abstract

The synthesis of 4-substituted amino-6-styryl/alkyl/aryl-1,2,4-triazin- 3,5(2H)diones (4a-d and 15) involving the cyclocondensation of N4-arylaminosemicarbazides(3a-d and 13) with some alpha-ketoacids is described. The behaviour of these triazinones towards amine, hydrazine, isothiocyanate, aromatic aldehyde and gl. acetic acid have been investigated. Structure elucidation of the new compounds has been carried out with the help of elemental analysis, IR, UV and 1H-NMR spectra. The antifungal activity of the prepared compounds has been assayed both in vitro and in vivo against some phytopathogenic fungi associated with wheat grains, were the compound 3b showed a high protection of the grains of wheat against the fungal infection.

摘要

描述了通过N4-芳基氨基氨基脲(3a-d和13)与一些α-酮酸的环缩合反应合成4-取代氨基-6-苯乙烯基/烷基/芳基-1,2,4-三嗪-3,5(2H)二酮(4a-d和15)的方法。研究了这些三嗪酮对胺、肼、异硫氰酸酯、芳香醛和冰醋酸的反应。借助元素分析、红外光谱、紫外光谱和1H-NMR光谱对新化合物进行了结构解析。对所制备的化合物针对与小麦籽粒相关的一些植物病原真菌进行了体内外抗真菌活性测定,其中化合物3b对小麦籽粒的真菌感染表现出高度保护作用。

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