Structure-guided design and biosynthesis of a novel FR-900098 analogue as a potent Plasmodium falciparum 1-deoxy-d-xylulose-5-phosphate reductoisomerase (Dxr) inhibitor

Ryan E. Cobb, Brian Bae, Zhi Li, Matthew A. Desieno, Satish K. Nair, Huimin Zhao

Research output: Contribution to journalArticlepeer-review

Abstract

We report here the enzymatic biosynthesis of FR-900098 analogues and establish an in vivo platform for the biosynthesis of an N-propionyl derivative FR-900098P. FR-900098P is found to be a significantly more potent inhibitor of Plasmodium falciparum 1-deoxy-d-xylulose 5-phosphate reductoisomerase (PfDxr) than the parent compound, and thus a more promising antimalarial drug candidate.

Original languageEnglish (US)
Pages (from-to)2526-2528
Number of pages3
JournalChemical Communications
Volume51
Issue number13
DOIs
StatePublished - Feb 14 2015

ASJC Scopus subject areas

  • Electronic, Optical and Magnetic Materials
  • General Chemistry
  • Ceramics and Composites
  • Metals and Alloys
  • Materials Chemistry
  • Surfaces, Coatings and Films
  • Catalysis

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