Structure-activity relationships of novel anti-malarial agents part 8. Effect of different central aryls in biarylacryloylaminobenzophenones on antimalarial activity.
Replacement of the 2,5-disubstituted furyl residue present in the known antimalarial agents 8 by other aryl residues resulted in a more or less reduced antimalarial activity in most cases. The only exemption was the 2,4-thienylene compound 11a displaying activity with an IC50 value of 120 nM. In conclusion, the 2,5-furylene compound 8e remains to represent the most active antimalarial agent in this series of farnesyltransferase inhibitors.
Wiesner
J
J
Biochemisches Institut der Justus-Liebig-Universität Giessen, Germany.
Mitsch
A
A
Altenkämper
M
M
Ortmann
R
R
Jomaa
H
H
Schlitzer
M
M
D019883:Alkyl and Aryl Transferases / Q000037:antagonists & inhibitors; D000818:Animals; D000962:Antimalarials / Q000737:chemistry* / Q000494:pharmacology*; D001577:Benzophenones / Q000737:chemistry* / Q000494:pharmacology*; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology; D051231:Farnesyltranstransferase; D007202:Indicators and Reagents; D008968:Molecular Conformation; D010963:Plasmodium falciparum / Q000187:drug effects / Q000254:growth & development; D013329:Structure-Activity Relationship
D000962:Antimalarials; D001577:Benzophenones; D004791:Enzyme Inhibitors; D007202:Indicators and Reagents; D019883:Alkyl and Aryl Transferases; D051231:Farnesyltranstransferase