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. 2004 Feb;48(2):525–532. doi: 10.1128/AAC.48.2.525-532.2004

TABLE 1.

Inhibition of different bacterial Phe-RS enzymes by the phenyl-thiazolylurea-sulfonamides

Enzyme and compound or drug IC50 (μM)a
E. coli H. influenzaeb S. pneumoniaeb
Phe-RS
    1 0.007 0.02 0.2
    2 0.008 0.008 0.2
    3 0.015 0.015 0.3
    4 0.015 0.015 0.05
    5 0.025 0.06 0.04
    6 0.02 0.02 0.2
    7 <0.005 0.01 0.3
Ile-RS
    Mupirocin 0.0014b 0.0014 0.0014
a

IC50s were determined for Phe-RS derived from different gram-negative and gram-positive pathogens. Inhibition of Ile-RS by mupirocin was measured in the presence of [14C]Ile instead of [14C]Phe; the results are included for comparison.

b

Values are the results of investigations performed using cell extracts.