کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10593270 | 981806 | 2013 | 6 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Design, synthesis and biological evaluation of α-substituted isonipecotic acid benzothiazole analogues as potent bacterial type II topoisomerase inhibitors
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
The discovery and optimisation of a new class of benzothiazole small molecules that inhibit bacterial DNA gyrase and topoisomerase IV are described. Antibacterial properties have been demonstrated by activity against DNA gyrase ATPase and potent activity against Staphylococcus aureus, Enterococcus faecalis, Streptococcus pyogenes and Haemophilus influenzae. Further refinements to the scaffold designed to enhance drug-likeness included analogues bearing an α-substituent to the carboxylic acid group, resulting in excellent solubility and favourable pharmacokinetic properties.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 23, Issue 24, 15 December 2013, Pages 6598-6603
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 23, Issue 24, 15 December 2013, Pages 6598-6603
نویسندگان
Lorraine C. Axford, Piyush K. Agarwal, Kelly H. Anderson, Laura N. Andrau, John Atherall, Stephanie Barker, James M. Bennett, Michael Blair, Ian Collins, Lloyd G. Czaplewski, David T. Davies, Carlie T. Gannon, Dushyant Kumar, Paul Lancett,