title: 2-Acylamino-5-chlorobenzophenones with enhanced selectivity towards malaria parasites.
abstract: Previously we described a series of 5-acylaminobenzophenones with considerable antimalarial activity. Unfortunately, most compounds also displayed high cytotoxicity resulting in low selectivity towards malaria parasites. Through the replacement of the 5-acylamino moiety by simple chlorine and further modifications of the 2-acylamino residue we could obtain inhibitors with improved selectivity towards malaria parasites combined with an acceptable reduction of antimalarial activity.
authors.affiliation: Institut für Pharmazeutische Chemie, Philipps-Universität Marburg, Marbacher Weg 6, Marburg 35032, Germany.
authors.forename: Swetlana
authors.initials: S
authors.lastname: Heinrich
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: Regina
authors.initials: R
authors.lastname: Ortmann
authors.forename: Hans-Martin
authors.initials: HM
authors.lastname: Dahse
authors.forename: Yulin
authors.initials: Y
authors.lastname: Wang
authors.forename: Michael
authors.initials: M
authors.lastname: Lanzer
authors.forename: Martin
authors.initials: M
authors.lastname: Schlitzer
mesh_terms: D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology* / Q000633:toxicity; D001577:Benzophenones / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology* / Q000633:toxicity; D006367:HeLa Cells; D006801:Humans; D020128:Inhibitory Concentration 50; D008288:Malaria / Q000469:parasitology*; D010963:Plasmodium falciparum / Q000187:drug effects*
chemical_list: D000962:Antimalarials; D001577:Benzophenones; C014317:2-amino-5-chlorobenzophenone