کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1395799 1501143 2014 14 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Design, synthesis and evaluation of second generation MurF inhibitors based on a cyanothiophene scaffold
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Design, synthesis and evaluation of second generation MurF inhibitors based on a cyanothiophene scaffold
چکیده انگلیسی


• Design, synthesis and evaluation of new series of cyanothiophene-based inhibitors of MurF.
• Low micromolar inhibitors of MurF from Escherichia coli and Streptococcus pneumoniae were obtained.
• The inhibitors show antibacterial activity against strains of Staphylococcus aureus and E. coli.

MurF ligase is a crucial enzyme that catalyses the ultimate intracellular step of bacterial peptidoglycan biosynthesis, and thus represents an attractive target for antibacterial drug discovery. We designed, synthesized and evaluated a new series of cyanothiophene-based inhibitors of MurF enzymes from Streptococcus pneumoniae and Escherichia coli. The target compounds had increased polarity compared to the first generation of inhibitors, with demonstrated enzyme inhibitory potencies in the low micromolar range. Furthermore, the best inhibitors displayed promising antibacterial activities against selected Gram-positive and Gram-negative strains. These results represent an important step towards the development of new antibacterial agents targeting peptidoglycan biosynthesis.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: European Journal of Medicinal Chemistry - Volume 73, 12 February 2014, Pages 83–96
نویسندگان
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