Synthesis and guanase inhibition studies of a novel ring-expanded purine analogue containing a 5:7-fused, planar, aromatic heterocyclic ring system.
Synthesis and guanase inhibition studies of a novel ring-expanded purine analogue containing a 5:7-fused, planar, aromatic heterocyclic ring system.
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含有 5:7 稠合平面芳香杂环系统的新型扩环嘌呤类似物的合成和鸟苷酶抑制研究。
DOI：
10.1016/s0960-894x(98)00672-6
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发表时间：
1998
影响因子：
2.7
通讯作者：
Hosmane,RS
中科院分区：
文献类型：
--
作者：
Rajappan,V;Hosmane,RS
报道了含有5：7-咪唑并[4，5-e][1，4]二氮杂环体系的新型平面、潜在芳香性、扩环的黄嘌呤类似物(1)的合成和鸟苷酶抑制研究。以1-苄基-5-硝基咪唑-4-羧酸(2)为起始原料，经6步反应合成了该化合物，并对其进行了生化筛选。化合物1是该酶的中等竞争性抑制物，其Ki值为2.2 7±0.6 6×10−4M。
The synthesis of a novel planar, potentially aromatic, ring-expanded xanthine analogue (1), containing the 5:7-fused imidazo[4,5-e][1,4]diazepine ring system, along with guanase inhibition studies are reported. The compound was synthesized in six steps, starting from 1-benzyl-5-nitroimidazole-4-carboxylic acid (2), and was biochemically screened against rabbit liver guanase. Compound 1 is a moderate competitive inhibitor of the enzyme with a Kiof 2.27 ± 0.66 × 10−4M.