吡酮酸类抗菌药物的研究——Ⅹ.1,7-双取代-6-氟-1,4-二氢-4-氧代喹啉-3-羧酸类化合物的合成与构效关系

STUDIES ON PYRIDONECARBOXYLIC ACIDS AS ANTIBACTERIAL AGENTS Ⅹ. SYNTHESIS AND STRUCTURE-ACTIVITY RELATIONSHIPS OF 1, 7-DISUBSTITUTED-6-FLUORO-1, 4- DIHYDRO-4-OXO- QUINOLINE-3-CARBOXYLIC ACIDS

摘要: 本文合成了一系列1-位含有呋喃环系,异噁唑环系及取代苯基,7-位为不同取代氨基的吡酮酸类化合物,测定了这些化合物对大肠杆菌ATCC-25922,金黄色葡萄球菌ATCC-6538 p的MIC值,并与双氟哌酸进行对照,探讨了这些化合物的构效关系。

Abstract: A series of pyridonecarboxylic acids were prepared. These compounds have different groups including substituted benzenes, fiwans and isoxazles at the 1-position, or different substituted amino groups at the 7-position. The in vitro antibacterial potencies of these compounds against E. coli. and S. aureus were tested, and structure- activity relationships were discussed.