title: New derivatives of quinoline-4-carboxylic acid with antiplasmodial activity.
abstract: New analogues of the recently published compound DDD107498 were prepared. Their activities were examined in vitro against the chloroquine-sensitive NF54 strain. The most active were also tested against the multiresistant K1strain of Plasmodium falciparum. A couple of the newly synthesized compounds showed promising antiplasmodial activity and selectivity. A single compound showed adequate reduction of parasitaemia (98.1%) in mice infected with Plasmodium berghei. Survival time was doubled compared to control. The results of the biological tests of the novel compounds were compared with the activities of drugs in use. Structure-activity relationships were discussed.
authors.affiliation: Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, University of Graz, Schubertstraße 1, A-8010 Graz, Austria.
authors.forename: Patrick
authors.initials: P
authors.lastname: Hochegger
authors.affiliation: Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, University of Graz, Schubertstraße 1, A-8010 Graz, Austria.
authors.forename: Johanna
authors.initials: J
authors.lastname: Faist
authors.affiliation: Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, University of Graz, Schubertstraße 1, A-8010 Graz, Austria.
authors.forename: Werner
authors.initials: W
authors.lastname: Seebacher
authors.affiliation: Institute for Chemistry and Technology of Materials (ICTM), University of Technology, Stremayrgasse 9, A-8010 Graz, Austria.
authors.forename: Robert
authors.initials: R
authors.lastname: Saf
authors.affiliation: Swiss Tropical and Public Health Institute, Socinstrasse 57, Basel CH-4002, Switzerland; University of Basel, Petersplatz 1, Basel 4003, Switzerland.
authors.forename: Pascal
authors.initials: P
authors.lastname: Mäser
authors.affiliation: Swiss Tropical and Public Health Institute, Socinstrasse 57, Basel CH-4002, Switzerland; University of Basel, Petersplatz 1, Basel 4003, Switzerland.
authors.forename: Marcel
authors.initials: M
authors.lastname: Kaiser
authors.affiliation: Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, University of Graz, Schubertstraße 1, A-8010 Graz, Austria. Electronic address: robert.weis@uni-graz.at.
authors.forename: Robert
authors.initials: R
authors.lastname: Weis
mesh_terms: D000818:Animals; D000962:Antimalarials / Q000737:chemistry / Q000494:pharmacology*; D021261:Parasitic Sensitivity Tests; D010963:Plasmodium falciparum / Q000187:drug effects*; D011804:Quinolines / Q000737:chemistry / Q000494:pharmacology*; D013057:Spectrum Analysis / Q000379:methods; D013329:Structure-Activity Relationship
chemical_list: D000962:Antimalarials; D011804:Quinolines; C059924:quinoline-4-carboxylic acid
keywords: Amides; Amines; Plasmodium falciparum; Quinolines