(+)-7-Deaza-5‘-noraristeromycin as an Anti-Trypanosomal Agent

The (+)-enantiomer of 7-deaza-5‘-noraristeromycin (4) has been found to show IC50 values ranging from 0.16 to 5.3 μM against four strains of African trypanosomes, one Trypanosoma brucei brucei isolate, and several clinical isolates of Trypanosoma brucei rhodesiense (agent of east African sleeping si...

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Bibliographic Details
Published in:Journal of medicinal chemistry 1997-02, Vol.40 (4), p.622-624
Main Authors: Seley, Katherine L, Schneller, Stewart W, Rattendi, Donna, Bacchi, Cyrus J
Format: Article
Language:English
Subjects:
Adenosine - analogs & derivatives
Adenosine - chemistry
Adenosine - pharmacology
Adenosylhomocysteinase
Animals
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antiparasitic agents
Antiviral Agents - chemistry
Antiviral Agents - pharmacology
Biological and medical sciences
Drug Design
Hydrolases - metabolism
Medical sciences
Pharmacology. Drug treatments
Stereoisomerism
Structure-Activity Relationship
Trypanocidal Agents - chemistry
Trypanocidal Agents - pharmacology
Trypanosoma brucei brucei
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Summary:The (+)-enantiomer of 7-deaza-5‘-noraristeromycin (4) has been found to show IC50 values ranging from 0.16 to 5.3 μM against four strains of African trypanosomes, one Trypanosoma brucei brucei isolate, and several clinical isolates of Trypanosoma brucei rhodesiense (agent of east African sleeping sickness), including a multidrug resistant clone of one isolate. While this compound was originally designed to inhibit S-adenosyl-l-homocysteine hydrolase, it has been found to have no effect on this enzyme.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm9605039