期刊
BIOCHEMICAL JOURNAL
卷 386, 期 -, 页码 127-135出版社
PORTLAND PRESS LTD
DOI: 10.1042/BJ20041378
关键词
antibacterial drug; 1-deoxy-D-xylulose 5-phosphate; 1-deoxy-D-Xylulose 5-phosphate reducto-isomerase; isoprenoid biosynthesis; malaria; 2-C-methyl-D-erythritol 4-phosphate
Isoprenoid biosynthesis via the methylerythritol phosphate pathway is a target against pathogenic bacteria and the malaria parasite Plasniodium falciparum. 4-(Hydroxyamino)-4-oxobutyl-phosphonic acid and 4-[hydroxy(methyl)amino]-4-oxobutyl phosphonic acid, two novel inhibitors of DXR (1-deoxy-D-xylulose 5-phosphate reducto-isomerase), the second enzyme of the pathway, have been synthesized and compared with fosmidomycin, the best known inhibitor of this enzyme. The latter phosphonohydroxamic acid showed a high inhibitory activity towards DXR, much like fosmidomycin, as well as significant antibacterial activity against Escherichia coli in tests on Petri dishes.
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