کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10588389 | 981454 | 2012 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
7-Azabicyclo[2.2.1]heptane as a scaffold for the development of selective sigma-2 (Ï2) receptor ligands
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
A series of N-substituted 7-azabicyclo[2.2.1]heptanes (12-17 and 22-25) and similarly substituted pyrrolidines (32-36 and 41-44) were synthesized as sterically-reduced, achiral analogs of adamantane- and trishomocubane-derived Ï ligands. In vitro competition binding assays against Ï receptors revealed that arylalkyl N-substituents conferred selectivity for the Ï2 subtype, while alicyclic or polycarbocyclic substituents imparted high affinity for both subtypes. The Ï2 binding and subtype selectivities of N-arylalkyl-7-azanorbornanes was generally greater than the analogously-substituted pyrrolidines, indicating that steric bulk and conformational restriction around the nitrogen atom are likely important for subtype discrimination.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 12, 15 June 2012, Pages 4059-4063
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 12, 15 June 2012, Pages 4059-4063
نویسندگان
Samuel D. Banister, Louis M. Rendina, Michael Kassiou,