کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1368789 | 981726 | 2016 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Discovery of benzamides as potent human β3 adrenergic receptor agonists
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
The paper will describe the synthesis and SAR studies that led to the discovery of benzamide (reverse amide) as potent and selective human β3-adrenergic receptor agonist. Based on conformationally restricted pyrrolidine scaffold we discovered earlier, pyrrolidine benzoic acid intermediate 22 was synthesized. From library synthesis and further optimization efforts, several structurally diverse reverse amides such as 24c and 24i were found to have excellent human β3-adrenergic potency and good selectivity over the β1 and β2 receptors. In addition to human β1, β2, β3 and hERG data, PK of selected compounds will be described.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 26, Issue 1, 1 January 2016, Pages 55–59
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 26, Issue 1, 1 January 2016, Pages 55–59
نویسندگان
Cheng Zhu, Nam F. Kar, Bing Li, Melissa Costa, Karen H. Dingley, Jerry Di Salvo, Sookhee N. Ha, Amanda L. Hurley, Xiaofang Li, Randy R. Miller, Gino M. Salituro, Mary Struthers, Ann E. Weber, Jeffrey J. Hale, Scott D. Edmondson,