کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1375701 | 981942 | 2009 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Discovery and optimization of highly ligand-efficient oxytocin receptor antagonists using structure-based drug design
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Discovery and optimization of highly ligand-efficient oxytocin receptor antagonists using structure-based drug design Discovery and optimization of highly ligand-efficient oxytocin receptor antagonists using structure-based drug design](/preview/png/1375701.png)
چکیده انگلیسی
A novel oxytocin antagonist was identified by ‘scaffold-hopping’ using Cresset FieldScreen molecular field similarity searching. A single cycle of optimization driven by an understanding of the key pharmacophoric elements required for activity led to the discovery of a potent, selective and highly ligand-efficient oxytocin receptor antagonist. Selectivity over vasopressin receptors was rationalized based on differences in the structure of the natural ligands.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 3, 1 February 2009, Pages 990–994
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 3, 1 February 2009, Pages 990–994
نویسندگان
Benjamin R. Bellenie, Nicholas P. Barton, Amanda J. Emmons, Jag P. Heer, Cristian Salvagno,