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[N2-芳基-三嗪酰阿莫西林及N2-苯基-N4-烷基（芳基）-三嗪酰阿莫西林的合成及其抗菌活性]

[Synthesis of N2-aryl-triazinoylamoxicillins and N2-phenyl-N4-alkyl (aryl)-triazinoylamoxicillins and their antibacterial activity].

作者信息

Zhao L X, Yao Q X

机构信息

Shenyang College of Pharmacy.

出版信息

Yao Xue Xue Bao. 1990;25(10):739-44.

PMID:2099587
Abstract

Sixteen derivatives of BL-P1908 were synthesized by reaction of 2-aryl-1, 2, 4-triazine -3, 5-dione -6-carboxylic acid, or 2-phenyl-4-alkyl (aryl) -1, 2, 4-triazine-3, 5-dione-6-carboxylic acid with amoxicillin. All of them are new compounds. Their chemical structures were determined by elemental analysis, IR and 1HNMR. Preliminary tests showed that all compounds have marked activities against standard G(+) and G(-) bacteria and five of them have certain characteristic of broad spectrum, but they have no activities against resistant strains S. aureus S1, E coli C1 and P. aeruginosa PS1 isolated from clinic.

摘要

通过2-芳基-1,2,4-三嗪-3,5-二酮-6-羧酸或2-苯基-4-烷基（芳基）-1,2,4-三嗪-3,5-二酮-6-羧酸与阿莫西林反应合成了16种BL-P1908的衍生物。它们均为新化合物。通过元素分析、红外光谱和核磁共振氢谱确定了它们的化学结构。初步试验表明，所有化合物对标准革兰氏阳性菌和革兰氏阴性菌均有显著活性，其中5种具有一定的广谱特性，但对从临床分离出的耐药菌株金黄色葡萄球菌S1、大肠杆菌C1和铜绿假单胞菌PS1无活性。

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