Polyamines with N-(3-phenylpropyl) substituents are effective competitive inhibitors of trypanothione reductase and trypanocidal agents

Several N-(3-phenylpropyl)-substituted spermidine and spermine derivatives were prepared and found to be potent competitive inhibitors of Trypanosoma cruzi trypanothione reductase (seven compounds with Ki values < 5 microM are described). The most effective inhibitor studied was compound 12 with...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2001-01, Vol.11 (2), p.251-254
Main Authors: ZHILI LI, FENNIE, Michael W, GANEM, Bruce, HANCOCK, Matthew T, KOBASLIJA, Muris, RATTENDI, Donna, BACCHI, Cyrus J, O'SULLIVAN, Mary C
Format: Article
Language:English
Subjects:
Animals
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antiparasitic agents
Binding, Competitive
Biological and medical sciences
Combinatorial Chemistry Techniques
Enzyme Inhibitors - chemical synthesis
Enzyme Inhibitors - chemistry
Enzyme Inhibitors - pharmacology
Inhibitory Concentration 50
Kinetics
Medical sciences
NADH, NADPH Oxidoreductases - antagonists & inhibitors
Pharmacology. Drug treatments
Polyamines - chemical synthesis
Polyamines - chemistry
Polyamines - pharmacology
Spermidine - analogs & derivatives
Spermine - analogs & derivatives
Structure-Activity Relationship
Trypanocidal Agents - chemical synthesis
Trypanocidal Agents - chemistry
Trypanocidal Agents - pharmacology
Trypanosoma brucei brucei - enzymology
Trypanosoma cruzi - enzymology
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Summary:Several N-(3-phenylpropyl)-substituted spermidine and spermine derivatives were prepared and found to be potent competitive inhibitors of Trypanosoma cruzi trypanothione reductase (seven compounds with Ki values < 5 microM are described). The most effective inhibitor studied was compound 12 with a Ki value of 0.151 microM. Six of the compounds described are also effective trypanocides with IC50 values < 1 microM.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(00)00643-0