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Issue 13, 2015
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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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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.

Graphical abstract: 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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Supplementary files

Article information


Submitted
18 Nov 2014
Accepted
20 Dec 2014
First published
22 Dec 2014

Chem. Commun., 2015,51, 2526-2528
Article type
Communication
Author version available

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

R. E. Cobb, B. Bae, Z. Li, M. A. DeSieno, S. K. Nair and H. Zhao, Chem. Commun., 2015, 51, 2526
DOI: 10.1039/C4CC09181G

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