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含手性肟基吡咯烷的新型氟喹诺酮类抗菌剂的合成与生物学评价

Syntheses and biological evaluation of new fluoroquinolone antibacterials containing chiral oxiimino pyrrolidine.

作者信息

Choi Dong Rack, Shin Jung Han, Yang Jin, Yoon Sue Hye, Jung Yong Ho

机构信息

Central Research Laboratory, Dong-Wha Pharm. Ind. Co. Ltd, Anyang, Kyunggi 430-017, South Korea.

出版信息

Bioorg Med Chem Lett. 2004 Mar 8;14(5):1273-7. doi: 10.1016/j.bmcl.2003.12.044.

DOI:10.1016/j.bmcl.2003.12.044
PMID:14980680
Abstract

The design and syntheses of new fluoroquinolone antibacterial agents having pyrrolidine ring at C-7 position are described. The pyrrolidine ring is optically active and possesses methyloxime functional group. Two of them have excellent in vitro antibacterial activities and pharmacokinetic profiles.

摘要

描述了在C-7位具有吡咯烷环的新型氟喹诺酮抗菌剂的设计与合成。该吡咯烷环具有光学活性并含有甲基肟官能团。其中两种具有优异的体外抗菌活性和药代动力学特征。

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引用本文的文献

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4-Ethoxy-imino-N'-methoxy-pyrrolidin-1-ium-3-carboximidamidium dichloride.4-乙氧基-亚氨基-N'-甲氧基-吡咯烷-1-鎓-3-羧亚胺二氯化物
Acta Crystallogr Sect E Struct Rep Online. 2009 Feb 21;65(Pt 3):o580. doi: 10.1107/S1600536809004772.
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tert-Butyl 3-carbamoyl-4-methoxy-imino-3-methyl-piperidine-1-carboxyl-ate.
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