کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1396332 1501183 2010 9 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Synthesis and in vitro antibacterial activity of fluoroquinolone derivatives containing 3-(N′-alkoxycarbamimidoyl)-4-(alkoxyimino) pyrrolidines
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Synthesis and in vitro antibacterial activity of fluoroquinolone derivatives containing 3-(N′-alkoxycarbamimidoyl)-4-(alkoxyimino) pyrrolidines
چکیده انگلیسی

A series of novel 7-[3-(N′-alkoxycarbamimidoyl)-4-(alkoxyimino)pyrrolidin-1-yl] fluoroquinolone derivatives were designed, synthesized and characterized by 1H NMR, MS and HRMS. These fluoroquinolones were screened for their in vitro antibacterial activity. Most of them exhibit good potency in inhibiting the growth of Staphylococcus aureus and Staphylococcus epidermidis (MIC: 0.06–4.00 μg/mL). The activity of compounds 33 and 43 against S. aureus including MRSA and S. epidermidis including MRSE (MIC: 0.06–0.125 μg/mL) is more than or comparable to the reference drugs levofloxacin and gemifloxacin. In addition, compound 33 is 32 and 16–32 fold more potent than both the reference drugs against Enterococcus faecium 08-7 and Klebsiella pneumoniae 09-22, respectively.

We report herein the synthesis of novel 7-[3-(N′-alkoxycarbamimidoyl)-4-(alkoxyimino)pyrrolidin -1-yl]fluquinolone derivatives 9–49. Most of the target compounds exhibit good potency in inhibiting the growth of S. aureus and S. epidermidis (MIC: 0.06–4.00 μg/mL). Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: European Journal of Medicinal Chemistry - Volume 45, Issue 11, November 2010, Pages 5498–5506
نویسندگان
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