Synthesis and evaluation of phosphonated N-heteroarylcarboxamides as DOXP-reductoisomerase (DXR) inhibitors

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Bodill, Taryn, Conibear, Anne, Blatch, Gregory ORCID: 0000-0003-0778-8577, Lobb, Kevin and Kaye, Perry T (2011) Synthesis and evaluation of phosphonated N-heteroarylcarboxamides as DOXP-reductoisomerase (DXR) inhibitors. Bioorganic and Medicinal Chemistry, 19 (3). pp. 1321-1327. ISSN 0968-0896

Abstract

Malaria continues to be an enormous health-threat in the developing world. Treatment is compounded by the phenomenon of drug resistance, and the development of novel therapeutics has become a research priority. Plasmodium falciparum (Pf) is the parasite responsible for the most dangerous form of human malaria, and the enzyme, 1-deoxy-1-D-xylulose 5-phosphate reductoisomerase (PfDXR) has recently been validated as a target for the design of potential antimalarial drugs.

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Item type	Article
URI	https://vuir.vu.edu.au/id/eprint/9014
DOI	10.1016/j.bmc.2010.11.062
Official URL	http://www.sciencedirect.com/science/article/pii/S...
Subjects	Historical > Faculty/School/Research Centre/Department > School of Biomedical and Health Sciences Historical > FOR Classification > 0601 Biochemistry and Cell Biology Historical > SEO Classification > 970111 Expanding Knowledge in the Medical and Health Sciences
Keywords	ResPubID23310, anti-malarial drugs, phosphonates; DOXP-reductoisomerase; enzyme inhibitors; in silico docking; saturation transfer difference (STD)
Citations in Scopus	23 - View on Scopus
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