کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1365747 981572 2006 7 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Design, synthesis, and anti-integrase activity of catechol–DKA hybrids
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Design, synthesis, and anti-integrase activity of catechol–DKA hybrids
چکیده انگلیسی

Following the discovery of diketoacid-containing compounds as HIV-1 integrase (IN) inhibitors, a plethora of new molecules have been published leading to four drugs under clinical trial. In an attempt to rationally design new dimeric diketoacids (DKAs) targeting two divalent metal ions on the active site of IN, potent inhibitors against purified IN were found with varied selectivity for strand transfer. In this context, we designed and synthesized a new series of catechol–DKA hybrids. These compounds presented micromolar anti-integrase activities with moderate antiviral properties.

We designed and synthesized a new series of catechol–diketoacid hybrids as HIV-1 integrase inhibitors. The strand transfer/3′-processing selectivity was affected by the presence of the catechol moiety. These compounds presented micromolar anti-integrase activities with moderate antiviral properties.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 14, Issue 9, 1 May 2006, Pages 2978–2984
نویسندگان
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