Inhibition of the synthesis of macromolecules in Escherichia coli by nitrofuran derivatives. I. (5-Nitro-2-furyl)vinylpyridines.

Abstract

It was found that (5-nitro-2-furyl) vinylpyridine derivatives inhibited the synthesis of bacterial macromolecules in intact cell and protoplast lysate systems of Escherichia coli K-12. Among the syntheses tested, DNA, RNA and protein syntheses were inhibited correlating to antibacterial activity but lipid synthesis was independent of it. In the derivatives active against the strain, most inhibited DNA and protein syntheses and some additionary RNA synthesis in intact cell system. In protoplast lysate system, these syntheses were markedly inhibited by all of them. The degree of the inhibition was usually more remarkable in DNA synthesis than in protein synthesis. One derivative, which was inactive against the strain but active against staphylococci, showed only the slight inhibition of DNA synthesis in intact cell system but did the marked inhibition of DNA and RNA syntheses in protoplast lysate system. The derivatives inactive against all bacteria tested showed no inhibition in intact cell system and no or relatively weak inhibition in protoplast lysate system. The results indicate that the inhibition of DNA synthesis is important for antibacterial activity of (5-nitro-2-furyl) vinylpyridine derivatives and the permeability of the derivatives into bacterial cells may have influence on the activity.