title: Antitrypanosomal activity of quaternary naphthalimide derivatives.
abstract: 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.
authors.affiliation: Institute of Pharmacy and Food Chemistry, University of Würzburg, Am Hubland, 97074 Wuerzburg, Germany.
authors.forename: Mathias
authors.initials: M
authors.lastname: Muth
authors.forename: Verena
authors.initials: V
authors.lastname: Hoerr
authors.forename: Melanie
authors.initials: M
authors.lastname: Glaser
authors.forename: Alicia
authors.initials: A
authors.lastname: Ponte-Sucre
authors.forename: Heidrun
authors.initials: H
authors.lastname: Moll
authors.forename: August
authors.initials: A
authors.lastname: Stich
authors.forename: Ulrike
authors.initials: U
authors.lastname: Holzgrabe
mesh_terms: 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
chemical_list: D007202:Indicators and Reagents; D053644:Naphthalimides; D014344:Trypanocidal Agents