کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
10591696 981760 2013 6 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Optimization of a novel potent and selective bacterial DNA helicase inhibitor scaffold from a high throughput screening hit
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Optimization of a novel potent and selective bacterial DNA helicase inhibitor scaffold from a high throughput screening hit
چکیده انگلیسی
Benzobisthiazole derivatives were identified as novel helicase inhibitors through high throughput screening against purified Staphylococcus aureus (Sa) and Bacillus anthracis (Ba) replicative helicases. Chemical optimization has produced compound 59 with nanomolar potency against the DNA duplex strand unwinding activities of both B. anthracis and S. aureus helicases. Selectivity index (SI = CC50/IC50) values for 59 were greater than 500. Kinetic studies demonstrated that the benzobisthiazole-based bacterial helicase inhibitors act competitively with the DNA substrate. Therefore, benzobisthiazole helicase inhibitors represent a promising new scaffold for evaluation as antibacterial agents.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 23, Issue 12, 15 June 2013, Pages 3481-3486
نویسندگان
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