Novel 4-Aminoquinolines Active against Chloroquine-Resistant and Sensitive P. falciparum Strains that also Inhibit Botulinum Serotype A

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• 作者：Bogdan A. Š ; olaja ; Dejan Opsenica ; Kirsten S. Smith ; Wilbur K. Milhous ; Nataš ; a Terzić ; Igor Opsenica ; James C. Burnett ; Jon Nuss ; Rick Gussio ; Sina Bavari
• 刊名：Journal of Medicinal Chemistry
• 出版年：2008
• 出版时间：August 14, 2008
• 年：2008
• 卷：51
• 期：15
• 页码：4388-4391
• 全文大小：125K
• 年卷期：v.51,no.15(August 14, 2008)
• ISSN：1520-4804

文摘

We report on the initial result of the coupling of 4-amino-7-chloroquinoline with steroidal and adamantane constituents to provide small molecules with excellent in vitro antimalarial activities (IC₉₀ (W2) down to 6.74 nM). The same entities also inhibit the botulinum neurotoxin serotype A light chain metalloprotease at low micromolar levels (7−31 μM). Interestingly, structural features imparting increased antimalarial activity also provide increased metalloprotease inhibition, thus allowing for simultaneous compound optimizations against distinct targets.