[Developments in anti-malaria agents: chemical data, structure-activity relationships].
Various features of the evolution of a few antimalarial drugs including amodiaquine, dihydrofolate-reductase inhibitors, and artemisinin are described. The mechanism of action of artemisinin is detailed to explain the information of the main metabolites and drug design of certain compounds. Structure-activity and structure-neurotoxicity relations are reported. A few examples of cyclic peroxycetal synthesis are given. Finally, trends in new and novel compounds are presented.
Debaert
M
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Pharmacie chimique - Chimie thérapeutique UFR de Pharmacie 3, rue du Professeur-Laguesse F 59045 Lille Cedex, France.
D000655:Amodiaquine / Q000737:chemistry; D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity; D037621:Artemisinins; D004351:Drug Resistance; D004365:Drugs, Chinese Herbal; D005493:Folic Acid Antagonists / Q000737:chemistry; D010963:Plasmodium falciparum / Q000187:drug effects; D012717:Sesquiterpenes / Q000737:chemistry; D013329:Structure-Activity Relationship
D000962:Antimalarials; D037621:Artemisinins; D004365:Drugs, Chinese Herbal; D005493:Folic Acid Antagonists; D012717:Sesquiterpenes; D000655:Amodiaquine; C031327:artemisinin