Synthesis, antimycobacterial and antibacterial evaluation of 1-[(1R, 2S)-2-fluorocyclopropyl]fluoroquinolone derivatives containing an oxime functional moiety
机构：[1]Zhengzhou Univ, New Drug Res & Dev Ctr, Sch Pharmaceut Sci, Zhengzhou 450001, Peoples R China;[2]Chinese Acad Med Sci, Inst Med Biotechnol, Beijing 100050, Peoples R China;[3]Peking Union Med Coll, Beijing 100050, Peoples R China;[4]Capital Med Univ, Beijing An Zhen Hosp, Dept Cardiac Surg, Beijing 100029, Peoples R China;临床科室心脏外科中心首都医科大学附属安贞医院[5]Capital Med Univ, Beijing Chest Hosp, Beijing TB & Thorac Tumor Res Inst, Dept Pharmacol,Beijing Key Lab Drug Resistance TB, Beijing 101149, Peoples R China
A series of novel 1-[(1R, 2S)-2-fluorocyclopropyl]fluoroquinolone derivatives 9a-d containing an oxime functional moiety were synthesized and evaluated for their biological activity. Our results reveal that 9a1 and 9b3 have good in vitro activity against MTB H37Rv ATCC 27294 (MIC: 0.25 mu g/mL) and two MDR-MTB clinical isolates (MICs: 0.065-0.125 mu g/mL). Most of 9a-d show potent activity against Escherichia coli and Klebsiella pneumoniae (MICs: <0.008-4 mu g/mL) except extended-spectrum beta-lactamase-producing strains. Especially, 9a1 and 9d4 possessing excellent in vitro activity against all of the fourteen Gram-positive strains including MRSA and MRSE (MICs: <0.008-2 mu g/mL) comparable to or better than the four reference drugs, show considerable in vivo efficacy against five Gram-negative and Gram-positive isolate strains (ED(50)s: 11.43-26.04 mg/kg). (C) 2014 Elsevier Masson SAS. All rights reserved.
基金：
National S&T Major Special Project on Major New Drug Innovations [2012ZX09301002-001-017/023, 2014ZX09507009-003]; NSFCNational Natural Science Foundation of China [81373267-003]
第一作者机构：[1]Zhengzhou Univ, New Drug Res & Dev Ctr, Sch Pharmaceut Sci, Zhengzhou 450001, Peoples R China;
通讯作者：
通讯机构：[2]Chinese Acad Med Sci, Inst Med Biotechnol, Beijing 100050, Peoples R China;[3]Peking Union Med Coll, Beijing 100050, Peoples R China;
推荐引用方式(GB/T 7714)：
Liu Hongmin,Huang Ju,Wang Jiayang,et al.Synthesis, antimycobacterial and antibacterial evaluation of 1-[(1R, 2S)-2-fluorocyclopropyl]fluoroquinolone derivatives containing an oxime functional moiety[J].EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY.2014,86:628-638.doi:10.1016/j.ejmech.2014.09.029.
APA：
Liu, Hongmin,Huang, Ju,Wang, Jiayang,Wang, Minghua,Liu, Mingliang...&Lu, Yu.(2014).Synthesis, antimycobacterial and antibacterial evaluation of 1-[(1R, 2S)-2-fluorocyclopropyl]fluoroquinolone derivatives containing an oxime functional moiety.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,86,
MLA：
Liu, Hongmin,et al."Synthesis, antimycobacterial and antibacterial evaluation of 1-[(1R, 2S)-2-fluorocyclopropyl]fluoroquinolone derivatives containing an oxime functional moiety".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 86.(2014):628-638
