Cannon M, Harford S, Davies J
Department of Biochemistry, King's College London, U.K.
J Antimicrob Chemother. 1990 Sep;26(3):307-17. doi: 10.1093/jac/26.3.307.
Chloramphenicol, thiamphenicol and three fluorinated derivatives, Sch 24893, Sch 25298 and Sch 25393, were studied with respect to inhibition of the growth of selected bacterial strains and cell-free translation systems. Thiamphenicol was the least potent inhibitor in the former experiments, but behaved similarly to chloramphenicol and Sch 25298 in the latter, thereby displaying selective inhibition of prokaryotic protein synthesis. Thiamphenicol and Sch 25298 were shown to be like chloramphenicol in inhibiting peptidyl transferase activity specifically on 70 S ribosomes, but the antibiotics bound to their common ribosomal-receptor site with different efficiencies in the order chloramphenicol greater than thiamphenicol greater than Sch 25298. Selected bacterial strains highly resistant to chloramphenicol and thiamphenicol because of chloramphenicol acetyltransferase production were, in contrast, highly sensitive to inhibition by the fluorinated antibiotics. Thus Sch 24893, Sch 25298 and Sch 25393 may have important uses in veterinary and clinical medicine.
对氯霉素、甲砜霉素以及三种氟化衍生物Sch 24893、Sch 25298和Sch 25393进行了研究，观察它们对选定细菌菌株生长和无细胞翻译系统的抑制作用。在前述实验中，甲砜霉素是效力最低的抑制剂，但在后者实验中其表现与氯霉素和Sch 25298相似，从而显示出对原核生物蛋白质合成的选择性抑制。结果表明，甲砜霉素和Sch 25298与氯霉素一样，能特异性抑制70 S核糖体上的肽基转移酶活性，但这些抗生素与它们共同的核糖体受体位点结合的效率不同，顺序为氯霉素＞甲砜霉素＞Sch 25298。相比之下，因产生氯霉素乙酰转移酶而对氯霉素和甲砜霉素高度耐药的选定细菌菌株，对氟化抗生素的抑制作用高度敏感。因此，Sch 24893、Sch 25298和Sch 25393可能在兽医学和临床医学中有重要用途。
