کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1371791 | 981856 | 2012 | 6 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
SAR of α7 nicotinic receptor agonists derived from tilorone: Exploration of a novel nicotinic pharmacophore
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: SAR of α7 nicotinic receptor agonists derived from tilorone: Exploration of a novel nicotinic pharmacophore SAR of α7 nicotinic receptor agonists derived from tilorone: Exploration of a novel nicotinic pharmacophore](/preview/png/1371791.png)
چکیده انگلیسی
The well-known interferon-inducer tilorone was found to possess potent affinity for the agonist site of the α7 neuronal nicotinic receptor (Ki = 56 nM). SAR investigations determined that both basic sidechains are essential for potent activity, however active monosubstituted derivatives can also be prepared if the flexible sidechains are replaced with conformationally rigidified cyclic amines. Analogs in which the fluorenone core is replaced with either dibenzothiophene-5,5-dioxide or xanthenone also retain potent activity.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 4, 15 February 2012, Pages 1633–1638
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 4, 15 February 2012, Pages 1633–1638
نویسندگان
Michael R. Schrimpf, Kevin B. Sippy, Clark A. Briggs, David J. Anderson, Tao Li, Jianguo Ji, Jennifer M. Frost, Carol S. Surowy, William H. Bunnelle, Murali Gopalakrishnan, Michael D. Meyer,