PMID: 7031248Dec 1, 1981Paper

Synthesis of some novel amodiaquine analogues as potential antimalarial and antifilarial compounds

Journal of Medicinal Chemistry
M L GoA S Wan

Abstract

Ten amodiaquine analogues, which are hybridized molecules of amodiaquine and diethylcarbamazine, were designed and synthesized. Six analogues, all bearing a basic tertiary amino function at their side chain, were active against Plasmodium berghei in mice and inhibited the mobility of adult worms and microfilariae of Breinlia booliati in vitro. They were inactive against Litomosoides carinii in Mastomys natalensis. The most active antimalarial compound, 7-chloro-4-[alpha-[[N-(4-methyl-1-piperazinyl)carbonyl]amino]-4-hydroxy-m-toluidino]quinoline, had twice the activity of amodiaquine. O-Methylation and N-ethylation generally reduced antimalarial activity. Analogues which lack a basic tertiary amino function at their side chain were also lacking in both antimalarial and antifilarial activities.

Citations

Mar 21, 1998·Pharmacology & Therapeutics·P M O'NeillB K Park
Mar 9, 2010·The American Journal of Tropical Medicine and Hygiene·Joseph KamgnoMichel Boussinesq
Mar 19, 2019·Journal of Labelled Compounds & Radiopharmaceuticals·Ruilian WuJurgen G Schmidt

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