کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1358888 | 981371 | 2015 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Rapid development of two factor IXa inhibitors from hit to lead
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
Two high-throughput screening hits were investigated for SAR against human factor IXa. Both hits feature a benzamide linked to a [6-5]-heteroaryl via an alkyl amine. In the case where this system is a benzimidazolyl-ethyl amine the binding potency for the hit was improved >500-fold, from 9 μM to 0.016 μM. For the other hit, which contains a tetrahydropyrido-indazole amine, potency was improved 20-fold, from 2 μM to 0.09 μM. X-ray crystal structures were obtained for an example of each class which improved understanding of the binding, and will enable further drug discovery efforts.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 25, Issue 11, 1 June 2015, Pages 2321–2325
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 25, Issue 11, 1 June 2015, Pages 2321–2325
نویسندگان
Dann L. Parker Jr., Shawn Walsh, Bing Li, Esther Kim, Aurash Sharipour, Cameron Smith, Yi-Heng Chen, Richard Berger, Bart Harper, Ting Zhang, Min Park, Min Shu, Jane Wu, Jiayi Xu, Sunita Dewnani, Edward C. Sherer, Alan Hruza, Paul Reichert,