کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10587031 | 981414 | 2010 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
1-Benzyl derivatives of 5-(arylamino)uracils as anti-HIV-1 and anti-EBV agents
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
Pyrimidine analogs have long found use over a broad chemotherapeutic spectrum. In an effort to further explore the antiviral potential of several uracil derivatives previously synthesized in our laboratories, a series of benzylated pyrimidines were designed and synthesized. Introduction of the benzyl residue onto the 5-phenylaminouracil scaffold was carried out using 2,4-bis(trimethylsilyloxy)pyrimidine with the corresponding benzyl bromides. Similarly, 1-benzyl-5-(benzylamino)- and 1-benzyl-5-(phenethylamino)uracils were obtained via amination of 1-benzyl-5-bromouracils with benzylamine or phenylethylamine. The results of the broad screen antiviral studies revealed that compounds 5 and 11 exhibit promising inhibitory activity against HIV-1 in CEM-SS culture. A 50% protective effect was observed at concentrations of 11.9 and 9.5 μÐ, respectively. Moreover, compounds 8 and 3 exhibited good inhibitory effects against EBV in ÐKÐТРcell culture with EC50 values of 2.3 and 12 μM, respectively. The synthesis and biological studies are detailed herein.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 18, Issue 23, 1 December 2010, Pages 8310-8314
Journal: Bioorganic & Medicinal Chemistry - Volume 18, Issue 23, 1 December 2010, Pages 8310-8314
نویسندگان
Mikhail S. Novikov, Robert W. Jr., Kartik Temburnikar, Anastasia L. Khandazhinskaya, Alexander V. Ivanov, Katherine L. Seley-Radtke,