کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1377596 | 981982 | 2007 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Scaffold hopping in the rational design of novel HIV-1 non-nucleoside reverse transcriptase inhibitors
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
High-throughput screening hit 1 was identified as a potent, broad-spectrum, non-nucleoside reverse transcriptase inhibitor (NNRTI) of HIV-1 replication. Analysis of the bound conformation of analogs of this inhibitor via molecular modeling and NMR contributed to the design of novel tertiary amide, carbamate, and thiocarbamate based NNRTIs.
Tetrazole thioacetanilides such as 12 were identified as potent NNRTIs via high-throughput screening. Analysis of the binding mode of these inhibitors permitted the successful scaffold hop to tertiary amides (23), carbamates (24), and thiocarbamates (26).Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 17, Issue 12, 15 June 2007, Pages 3362–3366
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 17, Issue 12, 15 June 2007, Pages 3362–3366
نویسندگان
Jeff A. O’Meara, Araz Jakalian, Steven LaPlante, Pierre R. Bonneau, René Coulombe, Anne-Marie Faucher, Ingrid Guse, Serge Landry, Jennifer Racine, Bruno Simoneau, Bounkham Thavonekham, Christiane Yoakim,