کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1367826 981650 2005 6 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Development of an oxazolopyridine series of dual thrombin/factor Xa inhibitors via structure-guided lead optimization
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Development of an oxazolopyridine series of dual thrombin/factor Xa inhibitors via structure-guided lead optimization
چکیده انگلیسی

Thrombin-inhibitor X-ray crystal structures, in combination with the installation of binding elements optimized within the pyrazinone series of thrombin inhibitors, were utilized to transform a weak triazolopyrimidine lead into a series of potent oxazolopyridines. A modification intended to attenuate plasma protein binding (i.e., conversion of the P3 pyridine to a piperidine) conferred significant factor Xa activity to this series. Ultimately, these dual thrombin/factor Xa inhibitors demonstrated excellent in vitro and in vivo anticoagulant efficacy.

Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 15, Issue 20, 15 October 2005, Pages 4411–4416
نویسندگان
, , , , , , , , , , , , , ,