In-vitro antibacterial activity of Sch 25393, a fluorinated analogue of thiamphenicol.
The in-vitro antibacterial activity of a fluorinated analogue of thiamphenicol, Sch 25393, has been evaluated in comparison with chloramphenicol and thiamphenicol. The substitution of an hydroxyl group at position 3 and of two atoms of chlorine with fluorine in the acyl side-chain improves remarkably the antibacterial activity of the compound against strains resistant to chloramphenicol and thiamphenicol because of the production of acetyltransferases, but not against strains resistant because of non-enzymatic mechanisms of resistance. Although itself resistant to the enzymatic inactivation, Sch 25393 is unable to inhibit the acetylation of chloramphenicol and thiamphenicol.
D000107:Acetylation; D000123:Acetyltransferases / Q000378:metabolism; D001419:Bacteria / Q000187:drug effects*; D002701:Chloramphenicol / Q000494:pharmacology*; D004926:Escherichia coli / Q000378:metabolism; D008826:Microbial Sensitivity Tests; D013839:Thiamphenicol / Q000031:analogs & derivatives* / Q000494:pharmacology*; D013997:Time Factors
D002701:Chloramphenicol; C035533:Sch 25393; D000123:Acetyltransferases; C041973:thiamphenicol acetyltransferase; D013839:Thiamphenicol