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.
In-vitro antibacterial activity of Sch 25393, a fluorinated analogue of thiamphenicol / G. Marca, R. Mattina, F. Dubini, G. Cocuzza. - In: JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY. - ISSN 0305-7453. - 13:5(1984 May), pp. 423-7-427. [10.1093/jac/13.5.423]
In-vitro antibacterial activity of Sch 25393, a fluorinated analogue of thiamphenicol
R. MattinaSecondo
;
1984
Abstract
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.Pubblicazioni consigliate
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