کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1360935 981452 2008 8 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Synthesis and activity of tetrapeptidic HTLV-I protease inhibitors possessing different P3-cap moieties
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Synthesis and activity of tetrapeptidic HTLV-I protease inhibitors possessing different P3-cap moieties
چکیده انگلیسی

The causative agent behind adult T-cell leukemia and tropical spastic paraparesis/HTLV-I-associated myelopathy is the human T-cell leukemia virus type 1 (HTLV-I). Tetrapeptidic HTLV-I protease inhibitors were designed on a previously reported potent inhibitor KNI-10516, with modifications at the P3-cap moieties. All the inhibitors showed high HIV-1 protease inhibitory activity (over 98% inhibition at 50 nM) and most exhibited highly potent inhibition against HTLV-I protease (IC50 values were less than 100 nM).

A series of novel tetrapeptidic HTLV-I protease inhibitors were prepared using an hydroxymethylcarbonyl isostere. Most inhibitors showed high HTLV-I and HIV-1 proteases inhibitory activity.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 16, Issue 10, 15 May 2008, Pages 5795–5802
نویسندگان
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