申请人:Chamberland Suzanne
公开号:US20080188499A1
公开(公告)日:2008-08-07
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).
本发明涉及公式(1.0)的化合物及其药物可接受的盐。本发明涉及化学实体,其中含有一种硝基呋喃或其他抗生素,与一种活性增强的远端环系统通过亚胺基团、乙烯基团、碳或杂环链或环直接连接,或亚胺基团或乙烯基团和碳或杂环链或环的组合连接。例如,硝基呋喃基团可以获得抗生素活性,而分子的其余结构则通过促进微生物的硝基还原、靶向细菌的摄取和/或细胞内渗透,同时对药理学性质(吸收、体内分布等)做出贡献,从而增强了抗微生物活性和/或扩大了抗微生物谱。