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

Authors
Wang, LJ Hosmane, RS
Citation
Lj. Wang et Rs. Hosmane, 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, BIOORG MED, 11(22), 2001, pp. 2893-2896
Citations number
43
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
11
Issue
22
Year of publication
2001
Pages
2893 - 2896
Database
ISI
SICI code
0960-894X(20011119)11:22<2893:AURANA>2.0.ZU;2-J
Abstract
The synthesis and enzyme inhibition studies of a novel ring-expanded acycli c nucleoside analogue 1 are reported. Compound 1 has been found to be a com petitive 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. (C) 2001 Elsevier S cience Ltd. All rights reserved.