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

doi:10.1039/c4cc09181g

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 journal › Article › peer-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. This journal is

Original language	English (US)
Pages (from-to)	2526-2528
Number of pages	3
Journal	Chemical Communications
Volume	51
Issue number	13
DOIs	https://doi.org/10.1039/c4cc09181g
State	Published - Feb 14 2015

ASJC Scopus subject areas

Catalysis
Electronic, Optical and Magnetic Materials
Ceramics and Composites
Chemistry(all)
Surfaces, Coatings and Films
Metals and Alloys
Materials Chemistry

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AU - Bae, Brian

AU - Li, Zhi

AU - Desieno, Matthew A.

AU - Nair, Satish K.

AU - Zhao, Huimin

N1 - Publisher Copyright: © The Royal Society of Chemistry.

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Y1 - 2015/2/14

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AB - 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. This journal is

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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

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