Synthesis and guanase inhibition studies of a novel ring-expanded purine analogue containing a 5:7-fused, planar, aromatic heterocyclic ring system

被引：11

作者：

Rajappan, V ^{[1
]}

Hosmane, RS ^{[1
]}

机构：

[1] Univ Maryland Baltimore Cty, Dept Chem & Biochem, Lab Drug Design & Synth, Baltimore, MD 21250 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 24期

关键词：

D O I：

10.1016/S0960-894X(98)00672-6

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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 K-i of 2.27 +/- 0.66 x 10(-4) M. (C) 1998 Elsevier Science Ltd. All rights reserved.

引用

页码：3649 / 3652

页数：4