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Screening of Potential Antibiotics, Inhibitors of the Nonmevalonate Pathway of Isoprenoid Biosynthesis (2-C-Methyl-D-Erythritol-2,4-Cyclodiphosphate Derivatives)

Abstract

The recently discovered nonmevalonate pathway of isoprenoid biosynthesis Is a prospective target in screening of new antibiotics. Because of the absence of the pathway in the animal cells, the specific inhibitors of the pathway will be a new class of antibiotics against many pathogens (which cause e.g. malaria, tuberculosis, etc), combining high efficiency and low toxicity. Several derivatives of 2-C-methyl-D-erythritol-2,4-cyclodiphosphate (MEC) were synthesized. 4-Phospho-methyl-D-erythritol-1,2-cyclophosphate, benzyl ether and benzyliden derivative of MEC inhibited the14C-MEC incorporation into isoprenoids of chromoplasts from red pepper with IC50 of 1.7-5 мМ. Some inhibition (about 10 %) was also observed with the use of dimethyl ether and isopropyliden derivative of MEC.

About the Authors

YU. V. Ershov
A. N. Bakh Institute of Biochemistry
Russian Federation


K. V. Mazikin
A. N. Bakh Institute of Biochemistry
Russian Federation


D. N. Ostrovsky
A. N. Bakh Institute of Biochemistry
Russian Federation


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Review

For citations:


Ershov Yu.V., Mazikin K.V., Ostrovsky D.N. Screening of Potential Antibiotics, Inhibitors of the Nonmevalonate Pathway of Isoprenoid Biosynthesis (2-C-Methyl-D-Erythritol-2,4-Cyclodiphosphate Derivatives). Antibiot Khimioter = Antibiotics and Chemotherapy. 2010;55(5-6):3-7. (In Russ.)

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ISSN 0235-2990 (Print)