Author/Authors :
Mirko Altenk?mper، نويسنده , , Benjamin Bechem، نويسنده , , Johann Perruchon، نويسنده , , Swetlana Heinrich، نويسنده , , Andrea M?del، نويسنده , , Regina Ortmann، نويسنده , , Hans-Martin Dahse، نويسنده , , Ellen Freunscht، نويسنده , , Yulin Wang، نويسنده , , Jennifer Rath، نويسنده , , August Stich، نويسنده , , Manuela Hitzler، نويسنده , , Peter Chiba، نويسنده , , Michael Lanzer، نويسنده , , Martin Schlitzer، نويسنده ,
Abstract :
Here, we describe a series of readily obtainable benzophenone derivatives with antimalarial and antitrypanosomal activity. The most active compounds display submicromolar activity against Plasmodium falciparum. Micromolar activity is obtained against Trypanosoma brucei. Main problem of the compounds is low selectivity. However, there are indications that separation of antimalarial and cytotoxic activity might by possible. In addition, some compounds inhibit human ABC transporter with nanomolar activity.
Keywords :
Trypanosoma brucei , Plasmodium falciparum , Multidrug resistance transporter , Sleeping sickness , malaria , Drug development