新型β-内酰胺类化合物对黄嘌呤氧化酶活性的体外影响。

Arlinda Bytyqi-Damoni, Hayriye Genç, Mustafa Zengin, Serap Beyaztas, Nahit Gençer, Oktay Arslan
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引用次数: 17

摘要

以n -甲基-3-氨基咔唑为原料,采用不同的醛合成咔唑取代亚胺(2a- 1)。亚胺类化合物与原位烯酮发生(2+2)环加成反应生成β-内酰胺类化合物(3a-l)。对从牛乳中纯化的黄嘌呤氧化酶(XO)的抑制剂β-内酰胺进行了测试。结果表明,这些化合物在低浓度下对XO有抑制作用,IC(50)值在21.65 ~ 58.04µM之间。对XO最有效的化合物是4-(4-氯苯基)-1-(9-乙基- 9h -carbazol-3-基)-3- phenylazetitin -2-one, IC(50)为21.65 μM。本文研究的内酰胺类药物显示出有效的XO抑制作用,与临床使用的别嘌呤醇相同。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
In vitro effect of novel β-lactam compounds on xanthine oxidase enzyme activity.

Carbazole substituted imines (2a-l) were prepared from N-methyl-3-amino carbazole with different aldehydes. The imines compounds undergo (2+2) cycloaddition reactions with in situ ketenes to produce β-lactam compounds (3a-l). The β-lactam compounds were tested as inhibitors of the xanthine oxidase (XO) purified from bovine milk. The results show that these compounds exhibit inhibitory effects on XO at low concentrations with IC(50) values ranging from 21.65 to 58.04 µM. The most effective compound for XO was 4-(4-chlorophenyl)-1-(9-ethyl-9H-carbazol-3-yl)-3-phenylazetidin-2-one with IC(50) of 21.65 μM. The lactams investigated here showed effective XO inhibitory effects, in the same range as the clinically used allopurinol.

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