کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1363970 | 981525 | 2009 | 6 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
3-Benzyl-1,3-oxazolidin-2-ones as mGluR2 positive allosteric modulators: Hit-to lead and lead optimization
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
The discovery, synthesis and SAR of a novel series of 3-benzyl-1,3-oxazolidin-2-ones as positive allosteric modulators (PAMs) of mGluR2 is described. Expedient hit-to-lead work on a single HTS hit led to the identification of a ligand-efficient and structurally attractive series of mGluR2 PAMs. Human microsomal clearance and suboptimal physicochemical properties of the initial lead were improved to give potent, metabolically stable and orally available mGluR2 PAMs.
The discovery, synthesis and SAR of a novel series of 3-benzyl-1,3-oxazolidin-2-ones as positive allosteric modulators (PAMs) of mGluR2 is described which led to potent, metabolically stable and orally available mGluR2 PAMs.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 9, 1 May 2009, Pages 2524–2529
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 9, 1 May 2009, Pages 2524–2529
نویسندگان
Allen J. Duplantier, Ivan Efremov, John Candler, Angela C. Doran, Alan H. Ganong, Jessica A. Haas, Ashley N. Hanks, Kenneth G. Kraus, John T. Lazzaro Jr., Jiemin Lu, Noha Maklad, Sheryl A. McCarthy, Theresa J. O’Sullivan, Bruce N. Rogers,