title: Antimalarial and antitrypanosomal activity of a series of amide and sulfonamide derivatives of a 2,5-diaminobenzophenone.
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.
authors.affiliation: Institut für Pharmazeutische Chemie, Philipps-Universität Marburg, Marbacher Weg 6, 35032 Marburg, Germany.
authors.forename: Mirko
authors.initials: M
authors.lastname: Altenkämper
authors.forename: Benjamin
authors.initials: B
authors.lastname: Bechem
authors.forename: Johann
authors.initials: J
authors.lastname: Perruchon
authors.forename: Swetlana
authors.initials: S
authors.lastname: Heinrich
authors.forename: Andrea
authors.initials: A
authors.lastname: Mädel
authors.forename: Regina
authors.initials: R
authors.lastname: Ortmann
authors.forename: Hans-Martin
authors.initials: HM
authors.lastname: Dahse
authors.forename: Ellen
authors.initials: E
authors.lastname: Freunscht
authors.forename: Yulin
authors.initials: Y
authors.lastname: Wang
authors.forename: Jennifer
authors.initials: J
authors.lastname: Rath
authors.forename: August
authors.initials: A
authors.lastname: Stich
authors.forename: Manuela
authors.initials: M
authors.lastname: Hitzler
authors.forename: Peter
authors.initials: P
authors.lastname: Chiba
authors.forename: Michael
authors.initials: M
authors.lastname: Lanzer
authors.forename: Martin
authors.initials: M
authors.lastname: Schlitzer
mesh_terms: D000577:Amides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D000962:Antimalarials / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001577:Benzophenones / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D008288:Malaria / Q000188:drug therapy / Q000469:parasitology; D021261:Parasitic Sensitivity Tests; D010963:Plasmodium falciparum / Q000187:drug effects* / Q000254:growth & development / Q000378:metabolism; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D014346:Trypanosoma brucei brucei / Q000187:drug effects* / Q000254:growth & development / Q000378:metabolism
chemical_list: C515585:2,5-diaminobenzophenone; D000577:Amides; D000962:Antimalarials; D001577:Benzophenones; D013449:Sulfonamides