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.
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.
Wiesner
Jochen
J
Biochemisches Institut der Universität Giessen, Friedrichstrasse 24, D-35249, Giessen, Germany.
Mitsch
Andreas
A
Jomaa
Hassan
H
Schlitzer
Martin
M
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
D000179:Acrylates; D000577:Amides; D000962:Antimalarials; D004791:Enzyme Inhibitors; D005663:Furans; D007202:Indicators and Reagents; D019883:Alkyl and Aryl Transferases; D051231:Farnesyltranstransferase