کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1361049 | 981456 | 2008 | 8 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Synthesis and GABAA receptor activity of oxygen-bridged neurosteroid analogs
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Synthesis and GABAA receptor activity of oxygen-bridged neurosteroid analogs Synthesis and GABAA receptor activity of oxygen-bridged neurosteroid analogs](/preview/png/1361049.png)
چکیده انگلیسی
Three analogs of neuroactive steroids were prepared (4–6) in which 1,11- or 11,19-oxygen bridges give a constrained conformation. Their 3D structures were obtained by ab initio calculations and in the case of 3α-hydroxy-11,19-epoxypregn-4-ene-20-one (4), confirmed by X-ray analysis. Biological activity of the synthetic steroids was assayed in vitro using t-[3H]butylbicycloorthobenzoate as radiolabeled ligand for the GABAA receptor. The activity of compound 4 was similar to that of allopregnanolone (1). 1α,11α-Epoxypregnanolone (6) was more active than pregnanolone (2).
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 16, Issue 7, 1 April 2008, Pages 3831–3838
Journal: Bioorganic & Medicinal Chemistry - Volume 16, Issue 7, 1 April 2008, Pages 3831–3838
نویسندگان
Lautaro D. Alvarez, Adriana S. Veleiro, Ricardo F. Baggio, María T. Garland, Valeria C. Edelsztein, Héctor Coirini, Gerardo Burton,