کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1369969 | 981799 | 2012 | 6 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Discovery of nor-seco himbacine analogs as thrombin receptor antagonists
دانلود مقاله + سفارش ترجمه
دانلود مقاله ISI انگلیسی
رایگان برای ایرانیان
کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
Discovery of a novel nor-seco himbacine analog as potent thrombin receptor (PAR-1) antagonist is described. Despite low plasma level, these new analogs showed excellent ex vivo efficacy in the monkey platelet aggregation assay. A potent hydroxy metabolite generated in vivo was identified as the agent responsible for the ex vivo efficacy. Following this discovery, the metabolite series was optimized to obtain analogs that showed very good ex vivo efficacy along with excellent pharmacokinetic profile in c. monkey.
Discovery of a nor-seco himbacine analog derived from the tetrahydrothiopyranyl himbacine derivative and identification of an active metabolite generated in vivo are described.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 7, 1 April 2012, Pages 2544–2549
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 7, 1 April 2012, Pages 2544–2549
نویسندگان
Mariappan V. Chelliah, Samuel Chackalamannil, Yan Xia, Keith Eagen, William J. Greenlee, Ho-Sam Ahn, Jacqueline Agans-Fantuzzi, George Boykow, Yunsheng Hsieh, Matthew Bryant, Tze-Ming Chan, Madhu Chintala,