Guanine, pyrazolo [3, 4-d] pyrimidine, and triazolo [4, 5-d] pyrimidine (8-azaguanine) phosphonate acyclic derivatives as inhibitors of purine nucleoside …

LM Beauchamp, JV Tuttle, ME Rodriguez…

Index: Beauchamp, Lilia M.; Tuttle, Joel V.; Rodriguez, Martha E.; Sznaidman, Marcos L. Journal of Medicinal Chemistry, 1996 , vol. 39, # 4 p. 949 - 956

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Citation Number: 56

Abstract

Phosphonate acyclic derivatives of guanines, pyrazolo [3, 4-d] pyrimidines, and triazolo [4, 5- d] pyrimidines (8-azaguanines) are inhibitors of the enzyme purine nucleoside phosphorylase (PNPase) with K i'values ranging from 0.05 to 1.6 μM. These compounds are enzymatically stable congeners of the potent PNPase inhibitor acyclovir diphosphate (53).