A Unique Ring-Expanded Acyclic Nucleoside Analogue that Inhibits Both Adenosine Deaminase (ADA) and Guanine Deaminase (GDA; Guanase): Synthesis and Enzyme Inhibition Studies of 4,6-Diamino-8H-1-hydroxyethoxymethyl-8-iminoimidazo[4,5-e][1,3]diazepine

Bioorganic & Medicinal Chemistry Letters
2001.0

Abstract

The synthesis and enzyme inhibition studies of a novel ring-expanded acyclic nucleoside analogue are reported. Compound has been found to be a competitive inhibitor of both adenosine deaminase (ADA) and guanine deaminase (GDA; guanase) with K(i)'s equal to 1.52+/-0.34 x 10(-4) M and 2.97+/-0.25 x 10(-5) M, respectively. Inhibition of two enzymes of purine metabolism may bear beneficial implications in antiviral therapy.

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