Antibacterial Activity of Chloramphenicol-Related Compounds toward a Chloramphenicol-Resistant Strains of Staphylococcus aureus

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Antibacterial activities of 146 chloramphenicol (CM) derivatives and analogues were investigated in a CM-resistant strain of Staphylococcus aureis. Seventeen compounds tested showed the same or much higher antibacterial activity when compared with CM. These compounds could be classified into two groups: The first group included ten compounds containing a benzoyl moiety in their structure and the remaining seven compounds did not possess that moiety. Compounds, which showed a fourfold higher antibacterial activity than CM, were six CM derivatives and two CM analogues. They were all included in the first group. Present and previous studies indicated that the most active CM-related compound was DL-α-dichloroacet-amido-α-methylene-P-nitropropiophenone, termed No. 61 (previously called CM 17). The mecha-nism of antibacterial activity of this compound was due to the fact that this was not inactivated be the CM acetyltransferase produced by the CM-resistant strain.