کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1372591 | 981871 | 2011 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Conformationally constrained analogs of BAY 59–3074 as novel cannabinoid receptor ligands
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Conformationally constrained analogs of BAY 59–3074 as novel cannabinoid receptor ligands Conformationally constrained analogs of BAY 59–3074 as novel cannabinoid receptor ligands](/preview/png/1372591.png)
چکیده انگلیسی
To obtain information on the pharmacophoric requirements of the CB1/CB2 partial agonist BAY 59–3074 we have synthesized a series of new conformationally constrained dibenzofuran (4a–d) and dibenzopyran analogs (5). All constrained analogs exhibited reduced binding affinity at both cannabinoid receptor subtypes, suggesting that planar conformations of these ligands are less favored by both receptors. We also found that 4c, 4d, and 5 exhibited 3- to 12-fold selectivity for hCB2 over rCB1 receptors and may serve as new chemotypes for the development of CB2-selective cannabinergics.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 19, 1 October 2011, Pages 5999–6002
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 19, 1 October 2011, Pages 5999–6002
نویسندگان
Heidi Teng, Ganesh A. Thakur, Alexandros Makriyannis,