(+)-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 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.
Seley
K L
KL
Department of Chemistry, Auburn University, Alabama 36849-5312, USA.
Schneller
S W
SW
Rattendi
D
D
Bacchi
C J
CJ
D000241:Adenosine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D043383:Adenosylhomocysteinase; D000818:Animals; D000998:Antiviral Agents / Q000737:chemistry* / Q000494:pharmacology; D015195:Drug Design; D006867:Hydrolases / Q000378:metabolism; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D014344:Trypanocidal Agents / Q000737:chemistry* / Q000494:pharmacology; D014346:Trypanosoma brucei brucei
C092763:7-deaza-5'-noraristeromycin; D000998:Antiviral Agents; D014344:Trypanocidal Agents; C030034:aristeromycin; D006867:Hydrolases; D043383:Adenosylhomocysteinase; D000241:Adenosine