Structure-activity relationships of novel anti-malarial agents. Part 2: cinnamic acid derivatives.
We have described compound 1 as a lead structure for a novel class of anti-malarial agents. Replacement of the 3-phenylpropionyl moiety of the lead structure 1 by a 4-propoxycinnamic acid residue resulted in a significant improvement in antimalarial activity. Compound 3q represents an important step in the development of lead structure 1 into an anti-malarial drug candidate.
Wiesner
J
J
Biochemisches Institut der Universitätsklinik Giessen, Germany.
Mitsch
A
A
Wissner
P
P
Jomaa
H
H
Schlitzer
M
M
D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis*; D002934:Cinnamates / Q000138:chemical synthesis / Q000493:pharmacokinetics*; D020650:Combinatorial Chemistry Techniques; D020128:Inhibitory Concentration 50; D008826:Microbial Sensitivity Tests; D010963:Plasmodium falciparum / Q000187:drug effects; D013329:Structure-Activity Relationship
D000962:Antimalarials; D002934:Cinnamates