Antitrypanosomal activity of quaternary naphthalimide derivatives

作者：Muth Mathias; Hoerr Verena; Glaser Melanie; Ponte Sucre Alicia; Moll Heidrun; Stich August; Holzgrabe Ulrike^*

来源：Bioorganic & Medicinal Chemistry Letters, 2007, 17(6): 1590-1593.

DOI：10.1016/j.bmcl.2006.12.088

• sleeping sickness
• Trypanosoma brucei
• quaternary and tertiary naphthalimides

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 bis-naphthalimides 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.

• 出版日期2007-3-15