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Retargeting azithromycin analogues to have dual-modality antimalarial activity.

Amy L BurnsBrad E SleebsGhizal SiddiquiAmanda E De PaoliDovile AndersonBenjamin LiffnerRichard HarveyJames G BeesonDarren J CreekChristopher D GoodmanGeoffrey I McFaddenDanny W Wilson
Published in: BMC biology (2020)
We show that azithromycin and analogues can rapidly kill malaria parasite asexual blood stages via a fast action mechanism. Development of azithromycin and analogues as antimalarials offers the possibility of targeting parasites through both a quick-killing and delayed-death mechanism of action in a single, multifactorial chemotype.
Keyphrases
  • plasmodium falciparum
  • molecular docking
  • structure activity relationship
  • molecular dynamics simulations
  • toxoplasma gondii