کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1369378 | 981775 | 2013 | 6 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
HCV NS5A replication complex inhibitors. Part 31: discovery of potent analogs with distinct core topologies
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
In a recent disclosure,1 we described the discovery of dimeric, prolinamide-based NS5A replication complex inhibitors exhibiting excellent potency towards an HCV genotype 1b replicon. That disclosure dealt with the SAR exploration of the peripheral region of our lead chemotype, and herein is described the SAR uncovered from a complementary effort that focused on the central core region. From this effort, the contribution of the core region to the overall topology of the pharmacophore, primarily vector orientation and planarity, was determined, with a set of analogs exhibiting <10 nM EC50 in a genotype 1b replicon assay.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 23, Issue 3, 1 February 2013, Pages 779–784
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 23, Issue 3, 1 February 2013, Pages 779–784
نویسندگان
Omar D. Lopez, Van N. Nguyen, Denis R. St. Laurent, Makonen Belema, Michael H. Serrano-Wu, Jason T. Goodrich, Fukang Yang, Yuping Qiu, Amy S. Ripka, Peter T. Nower, Lourdes Valera, Mengping Liu, Donald R. O’Boyle II, Jin-Hua Sun, Robert A. Fridell,