کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1376252 | 981954 | 2007 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
The role of fluorine substitution in the structure–activity relationships (SAR) of classical cannabinoids
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: The role of fluorine substitution in the structure–activity relationships (SAR) of classical cannabinoids The role of fluorine substitution in the structure–activity relationships (SAR) of classical cannabinoids](/preview/png/1376252.png)
چکیده انگلیسی
A facile synthesis of 1-fluoro-1-deoxy-Δ8-THC analogs with side chains seven carbons in length, in the alkane/ene/yne- series (6, 5, and 4), was achieved from 1-fluoro-3,5-dimethoxybenzene (1). In vitro studies show that substitution by a fluorine has a significant detrimental effect on CB1 binding which is supported by in vivo testing. The implications of these results on the SAR of classical cannabinoids are discussed.
Substitution of the phenolic hydroxyl group of THCs by a fluorine (4, 5, 6) has a significant detrimental effect on CB1 binding affinity.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 17, Issue 6, 15 March 2007, Pages 1504–1507
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 17, Issue 6, 15 March 2007, Pages 1504–1507
نویسندگان
Peter J. Crocker, Anu Mahadevan, Jenny L. Wiley, Billy R. Martin, Raj K. Razdan,