Antibacterial Activity of 3‐(l‐Methyl‐5‐Nitro‐2‐Imidazolylmethylideneamino)‐2‐Oxazolidinone

Abstract

The nitroimidazole tested is structurally related to furazolidone in that it contains a 5‐nitro‐imidazole instead of 5‐nitrofuran. The nitroimidazole was much less active in vitro than furazolidone against a spectrum of pathogenic organisms. However, it is active in vivo by oral administration against bacterial infections of mice and its low acute toxicity gives better therapeutic indices than are obtained with furazolidone. Plasma concentrations rise rapidly following oral administration of the nitroimidazole. Sufficient urinary excretion occurred to give significant activity in a mouse kidney infection incited by Staphylococcus aureus in which nitrofurantoin was inactive.

<i>In vitro</i> and <i>in vivo</i> Activity of 3-(1-Methyl 1-5-Nitro-2 Imidazolylmethylideneamino)-2-OxazoIidinone against <i>Pasteurella</i>

“…Most of the isolates are more sensitive to furazolidone than to MABN. However, these Pas- teurella strains are more sensitive to MABN than isolates of other genera that we have studied [1]. These findings were indicated by previous re search [1] and were not unexpected.…”

“…However, these Pas- teurella strains are more sensitive to MABN than isolates of other genera that we have studied [1]. These findings were indicated by previous re search [1] and were not unexpected. We did not expect the greater varia tion in sensitivity to MABN of the isolates in table I.…”

“…We have reported [1] that 3-(l-methyl)-5-nitro-2-imidazolylmethylideneamino)-2-oxazolidinone (MABN) is efficacious against a number of bacterial infections of mice. The in vivo activity of the compound was much better than would have been predicted from in vitro sensitivity of the bacterial pathogens.…”

“…Because of the structural relationship [1,4] of MABN and 3-(5-nitro-2-furfurylideneamino)-2-oxazolidinone, which is furazolidone, we have compared the two for in vitro activity against isolates of Pasteurella and Yersinia as well as for efficacy against animal infection caused by some of the strains.…”