title: Structure-activity relationships of novel anti-malarial agents. Part 7: N-(3-benzoyl-4-tolylacetylaminophenyl)-3-(5-aryl-2-furyl)acrylic acid amides with polar moieties.
abstract: In a previous report, we have provided evidence that novel anti-malarial compounds based on 2,5-diaminobenzophenone farnesyltransferase inhibitors might benefit from the presence of a polar moiety at the para position of the terminal phenyl of the arylfurylacryloyl partial structure. Here, we demonstrate that different moieties with hydrogen bond acceptor properties lead to equipotent or even improved anti-malarial activity in comparison to the nitro group described before.
authors.affiliation: Biochemisches Institut der Universität Giessen, Friedrichstrasse 24, D-35249, Giessen, Germany.
authors.forename: Jochen
authors.initials: J
authors.lastname: Wiesner
authors.forename: Andreas
authors.initials: A
authors.lastname: Mitsch
authors.forename: Hassan
authors.initials: H
authors.lastname: Jomaa
authors.forename: Martin
authors.initials: M
authors.lastname: Schlitzer
mesh_terms: D000179:Acrylates / Q000138:chemical synthesis* / Q000494:pharmacology*; D019883:Alkyl and Aryl Transferases / Q000037:antagonists & inhibitors; D000577:Amides / Q000138:chemical synthesis* / Q000494:pharmacology*; D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000494:pharmacology*; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology; D051231:Farnesyltranstransferase; D005663:Furans / Q000138:chemical synthesis* / Q000494:pharmacology*; D006860:Hydrogen Bonding; D007202:Indicators and Reagents; D010963:Plasmodium falciparum / Q000187:drug effects; D013329:Structure-Activity Relationship
chemical_list: D000179:Acrylates; D000577:Amides; D000962:Antimalarials; D004791:Enzyme Inhibitors; D005663:Furans; D007202:Indicators and Reagents; D019883:Alkyl and Aryl Transferases; D051231:Farnesyltranstransferase