Studies of N-hydroxy-N'-aminoguanidine derivatives by nitrogen-15 nuclear magnetic resonance spectroscopy and as ribonucleotide reductase inhibitors.

doi:10.1021/JM00363A021

Paper

Studies of N-hydroxy-N'-aminoguanidine derivatives by nitrogen-15 nuclear magnetic resonance spectroscopy and as ribonucleotide reductase inhibitors.

Published Sep 1, 1983 · A. W. Tai, E. Lien, E. Moore

Journal of medicinal chemistry

24

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0

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Abstract

Hydroxyguanidine, with the imino group of guanidine and the hydroxyamino group of hydroxyurea, has functional groups believed to be important for both anticancer and antiviral activities (Adamson, R.H. Nature (London) 1972, 236, 400-401). Three new N-hydroxy-N'-aminoguanidine derivatives have been synthesized and found to be 20-30 times more active than the hydroxyguanidine itself as inhibitors of ribonucleotide reductase from rat Novikoff tumors (Tai, W.A.; Lai, M.M.; Lien, E.J. "Novel N-Hydroxyguanidine Derivatives as Antiviral Agents", North American Medicinal Chemistry Symposium, University of Toronto, Toronto, Canada, June 20-24, 1982; Abstr, p 144). The character of the tautomeric equilibria, the pKa values, and the protonation sites of these hydroxyguanidine derivatives have been determined by 15N NMR spectroscopy.

Study Snapshot

N-hydroxy-N'-aminoguanidine derivatives show potential as antiviral agents, with 20-30 times higher activity than hydroxyguanidine itself, and their tautomeric equilibria, pKa values, and protonation sites can be determined by 15N NMR

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

Studies of N-hydroxy-N'-aminoguanidine derivatives by nitrogen-15 nuclear magnetic resonance spectroscopy and as ribonucleotide reductase inhibitors.

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