کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1364148 | 981530 | 2009 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
A new class of 5-HT2B antagonists possesses favorable potency, selectivity, and rat pharmacokinetic properties
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
We have been exploring the potential of 5-HT2B antagonists as a therapy for chronic heart failure. To assess the potential of this therapeutic approach, we sought compounds possessing the following attributes: (a) potent and selective antagonism of the 5-HT2B receptor, (b) low impact of serum proteins on potency, and (c) desirable pharmacokinetic properties. This Letter describes our investigation of a biphenyl benzimidazole class of compounds that resulted in 5-HT2B antagonists possessing the above attributes. Improving potency in a human serum albumin shift assay proved to be the most significant SAR discovery.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 8, 15 April 2009, Pages 2206–2210
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 8, 15 April 2009, Pages 2206–2210
نویسندگان
Neil Moss, Younggi Choi, Derek Cogan, Adam Flegg, Andreas Kahrs, Pui Loke, Orietta Meyn, Raj Nagaraja, Spencer Napier, Ashley Parker, J. Thomas Peterson, Philip Ramsden, Christopher Sarko, Donna Skow, Josh Tomlinson, Heather Tye, Mark Whitaker,