Antitrypanosomal activity of quaternary naphthalimide derivatives.
Sleeping sickness caused by Trypanosoma brucei gambiense and rhodesiense is fatal if left untreated. Due to the toxicity of drugs currently used and the emerging resistance against these drugs new lead compounds are urgently needed. Within the frame of a broad screening program for drugs with antitrypanosomal activity, some highly potent tertiary and quaternary mono- and bisnaphthalimides being active in the lower micromolar and nanomolar range of concentration have been identified. These compounds are easily available via a two- or three-step microwave-driven synthesis with high yield.
Muth
Mathias
M
Institute of Pharmacy and Food Chemistry, University of Würzburg, Am Hubland, 97074 Wuerzburg, Germany.
Hoerr
Verena
V
Glaser
Melanie
M
Ponte-Sucre
Alicia
A
Moll
Heidrun
H
Stich
August
A
Holzgrabe
Ulrike
U
D000818:Animals; D004353:Drug Evaluation, Preclinical; D006801:Humans; D007202:Indicators and Reagents; D051379:Mice; D053644:Naphthalimides / Q000138:chemical synthesis* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014344:Trypanocidal Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D014346:Trypanosoma brucei brucei / Q000187:drug effects
D007202:Indicators and Reagents; D053644:Naphthalimides; D014344:Trypanocidal Agents