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

  作者 Solaja, Bogdan A.;Opsenica, Dejan;Smith, Kirsten S.;Milhous, Wilbur K.;Terzic, Natasa;Opsenica, Igor;Burnett, James C.;Nuss, Jon;Gussio, Rick;Bavari, Sina;  
  选自 期刊  Journal of Medicinal Chemistry;  卷期  2008年51-15;  页码  4388-4391  
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[摘要]We report on the initial result of the coupling of 4-amino-7-chloroquinoline with steroidal and adamantane constituents to provide small mols. 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 mM). Interestingly, structural features imparting increased antimalarial activity also provide increased metalloprotease inhibition, thus allowing for simultaneous compd. optimizations against distinct targets.

 
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