کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1378254 | 981997 | 2007 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Synthesis and antibacterial activities of new quinolone derivatives utilizing 1-azabicyclo[1.1.0]butane
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
The ring-opening reactions of 1-azabicyclo[1.1.0]butane 3 with thiols 6a–f gave 3-sulfenylazetidine derivatives 7a–f in 50-92% yields. Treatment of 3 with aromatic amines 11a–e and dibenzylamine 11f in the presence of Mg(ClO4)2 afforded the corresponding 3-aminoazetidine derivatives 12a–f in 24–53% yields. These azetidine derivatives were introduced into the C7 position of a quinolone nucleus 8 to afford the corresponding fluoroquinolones 9a–f and 13a–f in 21–83% yields. Some of them exhibited superior antibacterial activity against quinolone-susceptible MRSA in comparison with clinically used fluoroquinolones, such as levofloxacin, ciprofloxacin, and gatifloxacin.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 17, Issue 4, 15 February 2007, Pages 942–945
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 17, Issue 4, 15 February 2007, Pages 942–945
نویسندگان
Yoshifumi Ikee, Kana Hashimoto, Masaaki Nakashima, Kazuhiko Hayashi, Shigeki Sano, Motoo Shiro, Yoshimitsu Nagao,