(+)-7-Deaza-5'-noraristeromycin as an anti-trypanosomal agent.

Abstract

The (+)-enantiomer of 7-deaza-5'-noraristeromycin (4) has been found to show IC50 values ranging from 0.16 to 5.3 microM 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.

• Authors: K L Seley, S W Schneller, D Rattendi, C J Bacchi
• Journal: Journal of medicinal chemistry (J Med Chem) Vol. 40 Issue 4 Pg. 622-4 (Feb 14 1997) ISSN: 0022-2623 [Print] United States
• PMID: 9046353 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• 7-deaza-5'-noraristeromycin
• Antiviral Agents
• Trypanocidal Agents
• aristeromycin
• Hydrolases
• Adenosylhomocysteinase
• Adenosine

Topics

• Adenosine (analogs & derivatives, chemistry, pharmacology)
• Adenosylhomocysteinase
• Animals
• Antiviral Agents (chemistry, pharmacology)
• Drug Design
• Hydrolases (metabolism)
• Stereoisomerism
• Structure-Activity Relationship
• Trypanocidal Agents (chemistry, pharmacology)
• Trypanosoma brucei brucei