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Synthesis and bioevaluation of hybrid 4-aminoquinoline triazines as a new class of antimalarial agents

  作者 Kumar, A; Srivastava, K; Kumar, SR; Puri, SK; Chauhan, PMS  
  选自 期刊  Bioorganic & Medicinal Chemistry Letters;  卷期  2008年18-24;  页码  6530-6533  
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[摘要]The emergence and rapid spread of chloroquine resistant strains of Plasmodium falciparum has dramatically reduced the chemotherapeutic options. Towards this goal, a series of new class of hybrid 4-aminoquinoline triazines were synthesized and screened against CQ sensitive strain 3D7 of P. falciparum in an in vitro model. Compounds 65 and 69 exhibited more than 99% suppression on day 4 and on day 6 post treatment, compound 69 showed impressive 99.11% suppression against CQ resistant strain N-67 of P. yoelii in an in vivo assay. (C) 2008 Elsevier Ltd. All rights reserved.

 
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