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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 
 
 
 
 

Novel C-2 substituted carbapenem derivatives. Part IV. Synthesis and biological activity of five membered heteroaromatic derivatives.

The synthesis, antibacterial activity, and stability to human dehydropeptidase-1 (DHP-1) of a novel series of (5R,6S)-6-[(1R)-1-hydroxyethyl]-2-heterocyclylcarbapen-2-em-3-carb oxylates are described. Of the compounds investigated 1,5-disubstituted pyrazol-3-yl and 3-substituted isoxazol-5-yl derivatives have the best combination of antibacterial activity and stability to DHP-1. They are particularly active against community-acquired respiratory tract pathogens and have stabilities to DHP-1 superior to that of meropenem.[1]

References

  1. Novel C-2 substituted carbapenem derivatives. Part IV. Synthesis and biological activity of five membered heteroaromatic derivatives. Branch, C.L., Burton, G., Clarke, G.J., Coulton, S., Douglas, J.D., Eglington, A.J., Guest, A.W., Hinks, J.D., Hird, N.W., Holland, R.K., Hunt, E., Knott, S.J., Moss, S.F., Naylor, A., Pearson, M.J., Takle, A.K. J. Antibiot. (1998) [Pubmed]
 
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