title: Structure-activity relationships of novel anti-malarial agents: 1. arylacyl and cyclohexylacyl derivatives of 5-amino-2-tolylacetylaminobenzophenone.
abstract: We have identified compound 1 as a lead structure of a novel class of anti-malarial agents. Here, we report on our continuing studies towards the establishment of structure-activity relationships by varying the terminal phenyl moiety and the alkyl linker of the acyl substituent at the 5-amino function of the benzophenone core structure. Most of the derivatives of our lead structure 1 essentially display the same anti-plasmodial activity as the lead.
authors.affiliation: Biochemisches Institut, Universitätsklinik Giessen, Giessen, Germany.
authors.forename: J
authors.initials: J
authors.lastname: Wiesner
authors.forename: A
authors.initials: A
authors.lastname: Mitsch
authors.forename: P
authors.initials: P
authors.lastname: Wissner
authors.forename: H
authors.initials: H
authors.lastname: Jomaa
authors.forename: M
authors.initials: M
authors.lastname: Schlitzer
mesh_terms: D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis / Q000737:chemistry*; D001577:Benzophenones / Q000737:chemistry*; D015195:Drug Design; D010963:Plasmodium falciparum / Q000187:drug effects; D013329:Structure-Activity Relationship
chemical_list: D000962:Antimalarials; D001577:Benzophenones