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
Year: 2014
Type: article
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.
Source: Chemical Communications
DOI: 10.1039/c4cc09181g
Authors: Ryan E. Cobb, Brian Bae, Zhi Li, Matthew A. DeSieno, Satish K. Nair, Huimin Zhao
Language: English
Subfield: Molecular Biology
Domain: Life Sciences
Open Access status: green
OpenAlex ID: W2046931315
