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1. 发明公开

KR1020090063869A 퀴놀린 카복실산 아마이드 유도체 또는 이의 약학적으로허용가능한 염, 이의 제조방법 및 이를 유효성분으로함유하는 항균 조성물 有权
标题翻译：喹啉 - 羧酸 - 酰胺衍生物或其药学上可接受的盐，其制备方法和含有它们作为活性成分的抗生素组合物
公开(公告)号：KR1020090063869A
公开(公告)日：2009-06-18
申请号：KR1020070131388
申请日：2007-12-14
申请人： 한국과학기술연구원 , 재단법인서울대학교산학협력재단
发明人： 신계정 , 문지연 , 배애님 , 김은경 , 서선희
IPC分类号： C07D215/38 , C07D215/48 , C07D401/12 , A61K31/47
摘要： An antibacterial composition containing a quinoline-carboxylic acid amide derivative or its pharmaceutically allowable salt is provided to suppress bacteria proliferation by inhibiting Fab I activation which is related to the last step of fatty acid biosynthesis. An antibacterial composition comprises a quinoline-carboxylic acid-amide derivative of the chemical formula 1 or its pharmaceutically allowable salt. A method for manufacturing the quinoline-carboxylic acid-amide derivative comprises: a step of reacting an aldehyde group of the chemical formula 2 with a phosphate, whose cyano group is substituted, to obtain a compound of the chemical formula 3; a step of performing intramolecular cyclization of the compound of the chemical formula 3 to obtain a quinoline compound of the chemical formula 4; a step of reacting the compound of the chemical formula 4 with a secondary amine to obtain a compound of the chemical formula 1(1a); and a step of reacting the compound of the chemical formula 1(1a) with an isocyanate to obtain the compound of the chemical formula 1.
摘要翻译：提供含有喹啉羧酸酰胺衍生物或其药学上可允许的盐的抗菌组合物，通过抑制与脂肪酸生物合成的最后步骤相关的Fab I激活来抑制细菌增殖。抗菌组合物包含化学式1的喹啉羧酸 - 酰胺衍生物或其药学上可允许的盐。喹啉羧酸 - 酰胺衍生物的制造方法包括：使化学式2的醛基与氰基取代的磷酸酯反应，得到化学式3的化合物的工序; 化学式3的化合物进行分子内环化的步骤，得到化学式4的喹啉化合物; 使化学式4的化合物与仲胺反应以获得化学式1（1a）的化合物的步骤; 以及使化学式1（1a）的化合物与异氰酸酯反应以获得化学式1的化合物的步骤。

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