کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1375873 | 981946 | 2009 | 4 صفحه PDF | دانلود رایگان |
A new series of 1β-methyl carbapenems possessing a 6,7-disubstituted imidazo[5,1-b]thiazol-2-yl group directly attached to the C-2 position of the carbapenem nucleus was prepared, and their activities against methicillin-resistant Staphylococcus aureus (MRSA) were evaluated. First, a benzyl moiety was introduced at the C-6 position of imidazo[5,1-b]thiazole attached to the carbapenem. These benzylated molecules showed potent anti-MRSA activity, but poor water solubility. In order to overcome this drawback, we designed and synthesized di- and tricationic carbapenems and finally discovered a novel carbapenem (15i), which exhibited excellent anti-MRSA activity and good water solubility.
A new series of 1β-methyl carbapenems possessing a 6,7,-disubstituted imidazo[5,1-b]thiazol-2-yl group was prepared. Among them, introduction of cationic benzyl moiety to the 6 position of imidazo[5,1-b]thiazole resulted in excellent anti-MRSA activity.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 2, 15 January 2009, Pages 447–450