کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1361673 | 981469 | 2011 | 7 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Synthesis and SAR studies on azetidine-containing dipeptides as HCMV inhibitors
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
SAR studies on an azetidine-containing dipeptide prototype inhibitor of HCMV are described. Three series of structurally modified analogues, involving substitutions at the N- and C-terminus, and at the C-terminal side-chain were synthesized and evaluated for antiviral activity. Aliphatic or no substituents at the C-carboxamide group, an aliphatic C-terminal side-chain, as well as a benzyloxycarbonyl moiety at the N-terminus were absolute requirements for anti-HCMV activity. The conformational restriction induced by the 2-azetidine residue into the dipeptide derivatives, identified by 1H NMR as a γ-type reverse turn, seems to have influence on the activity of these molecules.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 19, Issue 3, 1 February 2011, Pages 1155–1161
Journal: Bioorganic & Medicinal Chemistry - Volume 19, Issue 3, 1 February 2011, Pages 1155–1161
نویسندگان
Paula Pérez-Faginas, M. Teresa Aranda, M. Teresa García-López, Robert Snoeck, Graciela Andrei, Jan Balzarini, Rosario González-Muñiz,