Bonnefoy A, Girard A M, Agouridas C, Chantot J F
Antiinfective Research Department, Roussel UCLAF, Romainville, France.
J Antimicrob Chemother. 1997 Jul;40(1):85-90. doi: 10.1093/jac/40.1.85.
Ketolides belong to a new class of semi-synthetic 14-membered-ring macrolides, which differ from erythromycin A by having a 3-keto group instead of the neutral sugar L-cladinose. The ability of these molecules and their L-cladinose counterparts to induce MLS(B) resistance in staphylococci (one strain) and streptococci (two strains) was investigated using a disc agar susceptibility method as well as measuring induction kinetics. All 14- and 15-membered ring macrolides tested showed inducing activity. In contrast, ketolides were clearly unable to induce MLS(B) resistance, a result consistent with the high in-vitro activity of this new class of antibiotics against erythromycin A-inducible resistant bacteria.
酮内酯属于一类新型的半合成14元环大环内酯类抗生素,与红霉素A的不同之处在于其具有3-酮基而非中性糖L-克拉定糖。使用纸片琼脂扩散法并测量诱导动力学,研究了这些分子及其L-克拉定糖类似物在葡萄球菌(一株)和链球菌(两株)中诱导MLS(B)耐药性的能力。所有测试的14元和15元环大环内酯类抗生素均表现出诱导活性。相比之下,酮内酯显然无法诱导MLS(B)耐药性,这一结果与这类新型抗生素对红霉素A诱导性耐药菌的高体外活性相一致。