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7-(3-羟基-1,5-二氮杂环庚烷-1-胺基)-1-环丙基-6-氟-1,4-二氢-4氧代喹啉-3-羧酸及其类似物的合成与抗菌活性

Synthesis amd antibacterial activity of 7-(3-hydroxyl-1,5- diazacycloheptyl-1-yl)-1-cyclopropyl-6-fluoro-1,4-dihydro -4-oxo-3-quinolinecarboxylic acid and its analogues
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摘要 设计并合成了新化合物 7- (3-羟基 - 1,5 -二氮杂环庚烷 - 1-胺基 ) - 1-环丙基 - 6 -氟 - 1,4-二氢 - 4-氧代喹啉 - 3-羧酸 (5 a)及其类似物 5 b- 5 d,采用标准二倍稀释法测定了其对 2 6株有代表性的革兰氏阳性及革兰氏阴性菌的体外抗菌活性。结果表明化合物 5 a- 5 d对所测菌株的抑菌活性低于司帕沙星 ,而 5 a和 5 e则对革兰氏阳性菌金葡球菌有较高的活性 ,其最低抑菌浓度 MIC值为 0 .12 5 mg/ L。 hydroxyl 1,5 diazacycloheptyl 1 yl) 1 cyclopropy1 6 fluoro 1,4 dihydro 4 oxo 3 quinolinecarboxylic acid (5a) and its analogues 5b^5d have been synthesized and evaluated for their in vitro antibacterial activity against 26 strains of Gram positive and Gram negative organisms isolated by using standard agar dilution method. The results showed that antibacterial activity of the title compounds 5a^5d were lower than the sparfloxacin. While 5a and 5c showed higher potent against S.aureus than 5b and 5d. The MIC of 5a and 5c against S.aureus is 0.125mg/L.
出处 《中国抗生素杂志》 CAS CSCD 北大核心 2001年第6期440-442,450,共4页 Chinese Journal of Antibiotics
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