Synthesis and biological evaluation of phenolic Mannich bases of benzaldehyde and (thio) semicarbazone derivatives against the cysteine protease falcipain-2 and a …

A Chipeleme, J Gut, PJ Rosenthal, K Chibale

文献索引：Chipeleme, Alex; Gut, Jiri; Rosenthal, Philip J.; Chibale, Kelly Bioorganic and Medicinal Chemistry, 2007 , vol. 15, # 1 p. 273 - 282

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被引用次数: 74

摘要

A targeted series of phenolic Mannich bases of benzaldehyde and (thio) semicarbazone derivatives were synthesized and evaluated in vitro against the malarial cysteine protease falcipain-2 and a chloroquine resistant strain (W2) of Plasmodium falciparum. A novel series of 4-aminoquinoline semicarbazones were the most effective inhibitors of falcipain-2 (most potent inhibitor had IC50= 0.63 μM) while a bisquinoline semicarbazone compound 8f ...