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LM 427,一种新型螺哌啶基利福霉素:体外和体内研究

LM 427, a new spiropiperidylrifamycin: in vitro and in vivo studies.

作者信息

Della Bruna C, Schioppacassi G, Ungheri D, Jabès D, Morvillo E, Sanfilippo A

出版信息

J Antibiot (Tokyo). 1983 Nov;36(11):1502-6. doi: 10.7164/antibiotics.36.1502.

DOI:10.7164/antibiotics.36.1502
PMID:6317622
Abstract

The spiropiperidylrifamycin LM 427 (4-deoxo-3,4-[2-spiro-N-isobutyl-4-piperidyl]-(1H)-imidazo-(2,5-dihydro) rifamycin S) displays a broad spectrum of potent antibacterial activity in vitro. In vivo it is particularly effective in the therapy of experimental tubercular infections of mice. Three schedules of treatment were employed and the best results were obtained when intermittent administrations were used (ED50 of LM 427; 7 times lower than rifampicin). LM 427 is well distributed in tissues of mice and rats, with lung concentrations 10 to 20 times higher than plasma levels.

摘要

螺哌啶基利福霉素LM 427(4-脱氧-3,4-[2-螺-N-异丁基-4-哌啶基]-(1H)-咪唑-(2,5-二氢)利福霉素S)在体外具有广谱强效抗菌活性。在体内,它对小鼠实验性结核感染的治疗特别有效。采用了三种治疗方案,当使用间歇给药时获得了最佳结果(LM 427的半数有效剂量;比利福平低7倍)。LM 427在小鼠和大鼠组织中分布良好,肺组织浓度比血浆水平高10至20倍。

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