DXR Inhibition by Potent Mono- and Disubstituted Fosmidomycin Analogues
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چکیده
منابع مشابه
Synthesis and evaluation of ,-unsaturated -aryl-substituted fosmidomycin analogues as DXR inhibitors
Fosmidomycin, which acts through inhibition of 1-deoxy-D-xylulose phosphate reductoisomerase (DXR) in the nonmevalonate pathway, represents a valuable recent addition to the armamentarium against uncomplicated malaria. In this paper we describe the synthesis and biological evaluation of Eand Z-,-unsaturated -aryl-substituted analogues of FR900098, a fosmidomycin congener, utilizing a Stille ...
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The natural antibiotic fosmidomycin acts via inhibition of 1-deoxy-d-xylulose 5-phosphate reductoisomerase (DXR), an essential enzyme in the non-mevalonate pathway of isoprenoid biosynthesis. Fosmidomycin is active on Mycobacterium tuberculosis DXR (MtDXR), but it lacks antibacterial activity probably because of poor uptake. α-Aryl substituted fosmidomycin analogues have more favorable physicoc...
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ژورنال
عنوان ژورنال: Journal of Medicinal Chemistry
سال: 2013
ISSN: 0022-2623,1520-4804
DOI: 10.1021/jm4006498