Design of inhibitors against guanase: Synthesis and biochemical evaluation of analogues of azepinomycin

详细信息    查看全文

• 作者：Ravi K. Ujjinamatada ; Anila Bhan and Ramachandra S. Hosmane
• 关键词：Guanase (guanine deaminase) ; Inhibitors ; Azepinomycin analogues ; Synthesis ; Biochemical studies
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2006
• 出版时间：1 November 2006
• 年：2006
• 卷：16
• 期：21
• 页码：5551-5554
• 全文大小：137 K

文摘

As part of a program to design rational, mechanism-based inhibitors of guanase, we report here the synthesis and biochemical screening of two analogues of azepinomycin (1 and 2), a naturally occurring inhibitor of guanase, known to mimic the transition-state of the enzyme-catalyzed reaction. Our biochemical results show that compounds 1 and 2 are competitive inhibitors with K_i of 2.01 ± 0.16 × 10⁻⁵ and 5.36 ± 0.14 × 10⁻⁵ M, respectively.