Bacimethrin is isolated from Streptomyces albus. Bacimethrin is toxic to bacteria(e.g. B.cereus, E.coli and Proteus vulgaris) and yeast(e.g. Saccharomyces cerevisiae 7156, Cryplococcus neoformans and C. lauretii) growing in minimal media and has a minimum inhibitory concentration(MIC) in the low micromolar range. The toxicity can be reversed by adding thiamin to the culture medium.

Bacimethrin is inactive against sarcoma 180, leukaemia L-1210, sarcoma 37 and Ehrlich carcinoma, nor is it active against Newcastle disease virus and HeLa cells, or against T₂ phage of E.coli B2.

Bacimethrin is a substrate for the thiamin biosynthetic enzymes. It is an analog of the 4-amino-5-hydroxymethyl-2-methylpyrimidine(HMP) moiety of thiamine and inhibits the growth of Salmonella enterica.

The structure of bacimethrin is remarkably similar to those of 5-(hydroxy-methyl)cytosine and Bayer DG-428^646-648.The structural resemblance to vitamins B₁ and B₆ probably explains the fact that the antibiotic activity of bacimethrin is antagonized by vitamins B₁ and B₆.

Additional Information

Additional Information