1921
Volume 91, Issue 4
  • ISSN: 0002-9637
  • E-ISSN: 1476-1645

Abstract

Abstract.

Because of emerging resistance to existing drugs, new chemical classes of antimalarial drugs are urgently needed. We have rationally designed a library of compounds that were predicted to accumulate in the digestive vacuole and then decrystallize hemozoin by breaking the iron carboxylate bond in hemozoin. We report the synthesis of 16 naphthothiazolium salts with amine-bearing side chains and their activities against the erythrocytic stage of . KSWI-855, the compound with the highest efficacy against the asexual stages of , also had activity against gametocytes and activity against in a murine malaria model.

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2014-10-01
2017-11-20
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  • Received : 29 Sep 2013
  • Accepted : 06 May 2014

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