Structure-activity relationships of novel anti-malarial agents: 1. arylacyl and cyclohexylacyl derivatives of 5-amino-2-tolylacetylaminobenzophenone.
We have identified compound 1 as a lead structure of a novel class of anti-malarial agents. Here, we report on our continuing studies towards the establishment of structure-activity relationships by varying the terminal phenyl moiety and the alkyl linker of the acyl substituent at the 5-amino function of the benzophenone core structure. Most of the derivatives of our lead structure 1 essentially display the same anti-plasmodial activity as the lead.
Wiesner
J
J
Biochemisches Institut, Universitätsklinik Giessen, Giessen, Germany.
Mitsch
A
A
Wissner
P
P
Jomaa
H
H
Schlitzer
M
M
D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis / Q000737:chemistry*; D001577:Benzophenones / Q000737:chemistry*; D015195:Drug Design; D010963:Plasmodium falciparum / Q000187:drug effects; D013329:Structure-Activity Relationship
D000962:Antimalarials; D001577:Benzophenones