Wehrli W, Zimmermann W, Kump W, Tosch W, Vischer W, Zak O
Research Department, Ciba-Geigy Limited, Basel, Switzerland.
J Antibiot (Tokyo). 1987 Dec;40(12):1733-9. doi: 10.7164/antibiotics.40.1733.
CGP 4832 (5) is a new derivative of rifamycin S, showing a very high degree of activity against certain Gram-negative bacteria, with MICs as much as 400 times lower than those of rifampicin. CGP 4832 and rifampicin inhibit DNA-dependent transcription in vitro to a similar extent, which excludes any difference in their effect on the target enzyme. The most plausible explanation for the potent activity of CGP 4832 is that it penetrates into bacterial cells by way of a specific mechanism. This hypothesis is corroborated by the high rate of mutations leading to bacterial strains resistant against CGP 4832.
CGP 4832 (5)是利福霉素S的一种新衍生物，对某些革兰氏阴性菌显示出极高的活性，其最低抑菌浓度（MIC）比利福平低多达400倍。CGP 4832和利福平在体外对依赖DNA的转录的抑制程度相似，这排除了它们对靶酶的作用存在任何差异。对CGP 4832强大活性最合理的解释是它通过一种特定机制渗透到细菌细胞中。导致对CGP 4832耐药的细菌菌株的高突变率证实了这一假设。
