Title of article
Antimalarial and antitrypanosomal activity of a series of amide and sulfonamide derivatives of a 2,5-diaminobenzophenone Original Research Article
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 ,
Issue Information
روزنامه با شماره پیاپی سال 2009
Pages
8
From page
7690
To page
7697
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
Journal title
Bioorganic and Medicinal Chemistry
Serial Year
2009
Journal title
Bioorganic and Medicinal Chemistry
Record number
1306530
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