کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10591877 | 981767 | 2014 | 6 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Optimization of ketone-based P2Y12 receptor antagonists as antithrombotic agents: Pharmacodynamics and receptor kinetics considerations
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله

چکیده انگلیسی
Modification of a series of P2Y12 receptor antagonists by replacement of the ester functionality was aimed at minimizing the risk of in vivo metabolic instability and pharmacokinetic variability. The resulting ketones were then optimized for their P2Y12 antagonistic and anticoagulation effects in combination with their physicochemical and absorption profiles. The most promising compound showed very potent antiplatelet action in vivo. However, pharmacodynamic-pharmacokinetic analysis did not reveal a significant separation between its anti-platelet and bleeding effects. The relevance of receptor binding kinetics to the in vivo profile is described.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 24, Issue 13, 1 July 2014, Pages 2963-2968
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 24, Issue 13, 1 July 2014, Pages 2963-2968
نویسندگان
Fabrizio Giordanetto, Peter Bach, Fredrik Zetterberg, Thomas Antonsson, Ruth Bylund, Johan Johansson, Mikael Sellén, David Brown, Lotta HidestÃ¥hl, Pia Berntsson, Daniel Hovdal, Helen Zachrisson, Jan-Arne Björkman, J.J.J. van Giezen,