کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1370836 | 981830 | 2011 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Part 2: Design, synthesis and evaluation of hydroxyproline-derived α2δ ligands
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
Conformational constraint has been used to design a potent series of α2δ ligands derived from the readily available starting material (2S,4R)-hydroxy-l-proline. The ligands have improved physicochemistry and potency compared to their linear counterparts (described in our earlier publication) and the lead compound has been progressed to clinical development.
A series of proline-derived α2δ ligands has been designed through cyclisation of a lead series of N-alkylated glycines. Excellent levels of potency have been achieved and compound 18 has been progressed to clinical development.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 12, 15 June 2011, Pages 3767–3770
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 12, 15 June 2011, Pages 3767–3770
نویسندگان
David J. Rawson, Delphine Brugier, Anthony Harrison, Jo Hough, Julie Newman, Joe Otterburn, Graham N. Maw, Jenny Price, Lisa R. Thompson, Paul Turnpenny, Andrew N. Warren,