Synthesis and antimalarial activity of new isotebuquine analogues

OV Miroshnikova, TH Hudson, L Gerena…

文献索引：Miroshnikova, Olga V.; Hudson, Thomas H.; Gerena, Lucia; Kyle, Dennis E.; Lin, Ai J. Journal of Medicinal Chemistry, 2007 , vol. 50, # 4 p. 889 - 896

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被引用次数: 38

摘要

Amodiaquine (AQ) and tebuquine are 4-aminoquinoline antimalarials with Mannich base side chain and are highly effective against chloroquine (CQ)-resistant strains of Plasmodium falciparum. Clinical use of AQ has been severely restricted due to hepatoxicity and agranulocytosis side effects associated with its long term use. Lysosomal accumulation and bioactivation to generate reactive quinoneimine metabolite are implicated to be the cause ...