3-Amino-6-[2- (5-nitro-2-fury1) vinyl]-1, 2, 4-triazineおよびその誘導体の構造と生物活性相関薬剤耐性菌の感受性化作用を中心として

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タイトル別名
  • THE STRUCTURE AND BIOLOGICAL ACTIVITIES OF 3-AMINO-6- [2- (5-NITRO-2-FURYL) VINYL] -1, 2, 4-TRIAZINE AND ITS DERIVATIVES : ON THE CURING ACTION OF THE AGENT ON DRUG RESISTANT BACTERIA
  • 3-Amino-6- 2- 5-nitro-2-furyl vinyl -1 , 2 , 4-triazine オヨビ ソノ ユウドウタイ ノ コウゾウ ト セイブツ カッセイ ソウカン ヤクザイ タイセイキン ノ カンジュセイカ サヨウ オ チュウシン ト シテ

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説明

A curing action of three 5-nitrofuran compounds, possessing similar substituents with a triazine nucleus or its oxidized form at 2-position is described on some E. coli K-12 strains harboring R 100-1 and R100 factors. Treatment of R+cells (103-109 cells/ml) with sublethal concentrations of FT-H, FT, FT-Ac in Penassay broth (pH 7.6) led to the loss of part or all of these genetic elements. FTH and FT were shown to induce the elimination of drug resistance of R+cells more efficiently than FT-Ac. Appearance of drug-susceptible variants among survivors was observed around when the viable count of R+cells decreased 10-2-10-3 in 3-6 hrs. Several types of segregants were formed as well as R-cells. These segregants failed to transfer their R factors suggesting that transfer genes of their sex factors had mutated or had been deleted at least partly. Cmls variants gave no revertants to drug resistance. FT-H and FT were reduced metabolically by R+cells more rapidly than FT-Ac. Mutagenicities of these compounds were parallel to their metabolic reduction rates. It is concluded that all the biological activities of nitrofurans are derived from their metabolic reduction potential. It is also suggested that since the agent is not more toxic to R+cells than R- cells, the isolation of drug-susceptible variants under these conditions may be attributable to mutagenic actions of the agent.

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