کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1365035 | 981550 | 2008 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Structure-based design, synthesis, and biological evaluation of 1,1-dioxoisothiazole and benzo[b]thiophene-1,1-dioxide derivatives as novel inhibitors of hepatitis C virus NS5B polymerase
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Structure-based design, synthesis, and biological evaluation of 1,1-dioxoisothiazole and benzo[b]thiophene-1,1-dioxide derivatives as novel inhibitors of hepatitis C virus NS5B polymerase Structure-based design, synthesis, and biological evaluation of 1,1-dioxoisothiazole and benzo[b]thiophene-1,1-dioxide derivatives as novel inhibitors of hepatitis C virus NS5B polymerase](/preview/png/1365035.png)
چکیده انگلیسی
A novel series of HCV NS5B polymerase inhibitors comprising 1,1-dioxoisothiazoles and benzo[b]thiophene-1,1-dioxides were designed, synthesized, and evaluated. SAR studies guided by structure-based design led to the identification of a number of potent NS5B inhibitors with nanomolar IC50 values. The most potent compound exhibited IC50 less than 10 nM against the genotype 1b HCV polymerase and EC50 of 70 nM against a genotype 1b replicon in cell culture. The DMPK properties of selected compounds were also evaluated.
1,1-Dioxoisothiazole and benzo[b]thiophene-1,1-dioxide analogs were synthesized and tested as HCV NS5B polymerase inhibitors. Their PK properties were also evaluated.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 18, Issue 14, 15 July 2008, Pages 4181–4185
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 18, Issue 14, 15 July 2008, Pages 4181–4185
نویسندگان
Sun Hee Kim, Martin T. Tran, Frank Ruebsam, Alan X. Xiang, Benjamin Ayida, Helen McGuire, David Ellis, Julie Blazel, Chinh V. Tran, Douglas E. Murphy, Stephen E. Webber, Yuefen Zhou, Amit M. Shah, Mei Tsan, Richard E. Showalter, Rupal Patel,