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Carbocyclic and heterocyclic nitrofuran antibiotics and uses thereof

机译:碳环和杂环硝基呋喃抗生素及其用途

摘要

The present invention relates to compounds of the formula (1.0); and pharmaceutically acceptable salts of such compounds. The present invention relates to chemical entities containing a nitrofuran or other antibiotic linked to an activity enhancing distal ring system either directly or via an imine group, the vinyl group, the carbo- or hetero-cyclic chain or ring or a combination of an imine group or a vinyl group and a carbo- or hetero-cyclic chain or ring. Antibiotic activity is obtained, for example, by the nitrofuran moiety, while the remaining structure of the molecule contributes to additional antimicrobial activity and/or extends the antimicrobial spectrum of activity, by facilitating nitroreduction by microorganisms, uptake in target bacterial, and/or intracellular penetration, while also contributing to pharmacological properties (absorption, body distribution, and others).
机译:本发明涉及式(1.0)的化合物;以及此类化​​合物的可药用盐。本发明涉及直接或通过亚胺基,乙烯基,碳或杂环链或环或亚胺基的组合连接到增强活性的远端环系统上的硝基呋喃或其他抗生素的化学实体。或乙烯基和碳或杂环链或环。抗生素活性例如通过硝基呋喃部分获得,而分子的其余结构通过促进微生物的硝化还原,靶细菌的摄取和/或细胞内,有助于增加抗菌活性和/或扩展抗菌谱。渗透,同时也有助于药理特性(吸收,身体分布等)。

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