[Omega-aminoacyl compounds against malaria].
Investigations on diphenylthioether derivatives led to compounds with a high antimalarial (P. berghei) activity. 58 new compounds were synthetisized in order to study structure-efficacy relationships. General formula: Efficacy was optimal in compounds with R1 = NO2. Some of such compounds were at least half as effective as chloroquine and fully effective against drug resistant strains of P. berghei. But also other radicals proved to be suitable as long as S was not replaced by O. But two diphenylthioether derivatives (R1 = NO2 resp. CN) were found to be mutagenic in Salmonella/Microsome Ames test. Replacement of S by O caused a loss of mutagenicity but also a markedly drop of antimalarial activity.
D000577:Amides / Q000627:therapeutic use*; D000818:Animals; D000962:Antimalarials / Q000627:therapeutic use*; D004352:Drug Resistance, Microbial; D008288:Malaria / Q000188:drug therapy* / Q000469:parasitology; D008297:Male; D051379:Mice; D010647:Phenyl Ethers / Q000627:therapeutic use*; D010962:Plasmodium berghei / Q000187:drug effects; D013329:Structure-Activity Relationship; D013440:Sulfides / Q000627:therapeutic use
D000577:Amides; D000962:Antimalarials; D010647:Phenyl Ethers; D013440:Sulfides
Untersuchungen an malariawirksamen omega-Aminoacyl-Verbindungen.