کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1371994 | 981863 | 2009 | 6 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Spiropiperidine CCR5 antagonists
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
A novel series of CCR5 antagonists has been identified, utilizing leads from high-throughput screening which were further modified based on insights from competitor molecules. Lead optimization was pursued by balancing opposing trends of metabolic stability and potency. Selective and potent analogs with good pharmacokinetic properties were successfully developed.
The discovery of a novel series of CCR5 small molecule antagonists is described. Lead optimization was pursued by balancing opposing trends of metabolic stability and potency. Selective and potent analogs with good pharmacokinetic properties were developed as exemplified by compound 19.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 18, 15 September 2009, Pages 5401–5406
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 18, 15 September 2009, Pages 5401–5406
نویسندگان
David M. Rotstein, Stephen D. Gabriel, Ferenc Makra, Lubov Filonova, Shelley Gleason, Christine Brotherton-Pleiss, Lina Q. Setti, Alejandra Trejo-Martin, Eun Kyung Lee, Surya Sankuratri, Changhua Ji, Andre deRosier, Marianna Dioszegi, Gabrielle Heilek,