کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1378002 | 981992 | 2007 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
High-throughput screening affords novel and selective trypanothione reductase inhibitors with anti-trypanosomal activity
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: High-throughput screening affords novel and selective trypanothione reductase inhibitors with anti-trypanosomal activity High-throughput screening affords novel and selective trypanothione reductase inhibitors with anti-trypanosomal activity](/preview/png/1378002.png)
چکیده انگلیسی
Trypanothione reductase (TR), an enzyme that buffers oxidative stress in trypanosomatid parasites, was screened against commercial libraries containing approximately 134,500 compounds. After secondary screening, four chemotypes were identified as screening positives with selectivity for TR over human glutathione reductase. Thirteen compounds from these four chemotypes were purchased, and their in vitro activity against TR and Trypanosoma brucei is described.
Trypanothione reductase (TR) was screened against 134,500 compounds. Four chemotypes were selective for TR over human glutathione reductase. The in vitro activity of 13 purchased compounds against TR and Trypanosoma brucei is summarized.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 17, Issue 5, 1 March 2007, Pages 1280–1283
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 17, Issue 5, 1 March 2007, Pages 1280–1283
نویسندگان
Derek C. Martyn, Deuan C. Jones, Alan H. Fairlamb, Jon Clardy,