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新型氟喹诺酮类药物拉斯库氟沙星（KRP-AM1977）的活性与抗菌谱

Activities and Spectrum of the Novel Fluoroquinolone Lascufloxacin (KRP-AM1977).

作者信息

Kishii Ryuta, Yamaguchi Yuko, Takei Masaya

机构信息

Watarase Research Center, Kyorin Pharmaceutical Co., Ltd., Tochigi, Japan

Watarase Research Center, Kyorin Pharmaceutical Co., Ltd., Tochigi, Japan.

出版信息

Antimicrob Agents Chemother. 2017 May 24;61(6). doi: 10.1128/AAC.00120-17. Print 2017 Jun.

DOI:10.1128/AAC.00120-17
PMID:28320717
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC5444182/
Abstract

Lascufloxacin exhibited a broad spectrum of activity against various clinical isolates. Furthermore, lascufloxacin showed the most potent activity against Gram-positive bacteria among the quinolones tested and incomplete cross-resistance against existing quinolone-resistant strains. Enzymatic analysis indicated that lascufloxacin had potent inhibitory activity against both wild-type and mutated target enzymes. These results suggest that lascufloxacin may be useful in treating infections caused by various pathogens, including quinolone-resistant strains.

摘要

拉舒氟沙星对各种临床分离株表现出广谱活性。此外，在测试的喹诺酮类药物中，拉舒氟沙星对革兰氏阳性菌显示出最强的活性，并且对现有的喹诺酮耐药菌株具有不完全交叉耐药性。酶分析表明，拉舒氟沙星对野生型和突变型靶酶均具有强大的抑制活性。这些结果表明，拉舒氟沙星可能有助于治疗由各种病原体引起的感染，包括喹诺酮耐药菌株。