The bisnaphthalimides as new active lead compounds against Plasmodium falciparum

作者：Tischer Maximilian; Sologub Ludmilla; Pradel Gabriele^*; Holzgrabe Ulrike

来源：Bioorganic & Medicinal Chemistry, 2010, 18(9): 2998-3003.

DOI：10.1016/j.bmc.2010.03.067

• Malaria
• Plasmodium falciparum
• Bisquaternary bisnaphthalimides

The bisquaternary bisnaphthalimides are a versatile class of compounds being active against the malaria parasite Plasmodium falciparum in the lower nanomolar range of concentration combined with no cytotoxicity. The series of compounds is designed as choline analogues and interfering agents of the phosphatidylcholine biosynthesis. The qualitative analysis of the structure-activity relationships (SAR) revealed the importance of a long methylene middle chain of at least 8 methylene groups between the two bisquaternary naphthalimides or a monoquaternary naphthalimide consisting of a long alkyl chain attached to the positively charged nitrogen atom. Since the SARs are different from reported biscationic antimalarial drugs the mode of action remains to be elucidated.

• 出版日期2010-5-1