کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10582626 | 981075 | 2012 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
The design and synthesis of potent, selective benzodiazepine sulfonamide bombesin receptor subtype 3 (BRS-3) agonists with an increased barrier of atropisomerization
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
Bombesin receptor subtype 3 (BRS-3) is an orphan G-protein coupled receptor expressed primarily in the hypothalamus which plays a role in the onset of both diabetes and obesity. We report herein our progress made towards identifying a potent, selective bombesin receptor subtype-3 (BRS-3) agonist related to the previously described MK-77251 Chobanian et al. (2012) that would prevent atropisomerization through the increase of steric bulk at the C-2 position. This would thereby make clinical development of this class of compounds more cost effective by inhibiting racemization which can occur over long periods of time at room/elevated temperature.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 20, Issue 9, 1 May 2012, Pages 2845-2849
Journal: Bioorganic & Medicinal Chemistry - Volume 20, Issue 9, 1 May 2012, Pages 2845-2849
نویسندگان
Harry R. Chobanian, Yan Guo, Ping Liu, Thomas J. Jr., Marc Chioda, Linda Chang, Theresa M. Kelly, Yanqing Kan, Oksana Palyha, Xiao-Ming Guan, Donald J. Marsh, Joseph M. Metzger, Katie Raustad, Sheng-Ping Wang, Alison M. Strack, Judith N. Gorski,