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.
Publication types
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Adenosine Deaminase Inhibitors*
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Animals
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Azepines / chemical synthesis*
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Azepines / pharmacology
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Enzyme Inhibitors / chemical synthesis*
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Enzyme Inhibitors / pharmacology
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Guanine Deaminase / antagonists & inhibitors*
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Imidazoles / chemical synthesis*
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Imidazoles / pharmacology
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Liver / drug effects
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Liver / enzymology
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Rabbits
Substances
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4,6-diamino-8H-1-hydroxyethoxymethyl-8-iminoimidazo(4,5-e)(1,3)diazepine
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Adenosine Deaminase Inhibitors
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Azepines
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Enzyme Inhibitors
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Imidazoles
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Guanine Deaminase